CJC-1295 is a synthetic peptide which acts as a growth hormone secretagogue. CJC-1295 is also referred to as DAC:GRF, this stands for drug affinity complex: growth hormone releasing factor. CJC-1295 is a growth hormone (GH) and insulin-like growth factor 1 (IGF-1) releasing peptide with a long half-life. Administration of CJC-1295 is an incredibly effective method to increase the natural release of GH and elevate IGF-1 levels.
What is CJC-1295?
CJC-1295 is a synthetic analogue of the naturally occurring peptide, growth hormone-releasing hormone (GHRH) also known as growth hormone-releasing factor (GRF). CJC was developed by CONJUCHEM Biotechnologies Inc. GHRH is a 44 amino acid peptide which is required for the natural pulsatory secretion of GH; amino acids 1-29 are responsible for its biological activity. Exogenous application of Growth Hormone is associated with several negative side effects and it is believed that these side effects can be circumvented by using growth hormone secretagogues such as GRF. This is because of the growth hormone secretagogue’s more natural pulsatory release of GH. However, GRF has far too short of a half life to see clinically relevant elevations in GH and IGF. CJC-1295 was derived from the modification of GRF1-29 and selected for further research due to its long half-life. CJC provides the natural pulsatory release of GH and IGF-1 like GRF, but for longer periods of time which makes it a great candidate for therapeutic use.
CJC-1295 is GRF1-29 with a modification to four amino acids. This prevents biological degradation of the peptide. This is done by resisting proteolytic cleavage by proteolytic enzymes like dipeptidyl peptidase-4 (PPD-4), which is known to cleave growth factors. The modification to the four amino acids is know as Drug Affinity Complex TM (DAC). DAC is a peptide drug technology developed by CONJUCHEM Biotechnologies Inc. DAC modifies 4 amino acid positions that will still allow for biological activity of the original peptide, while preventing cleavage. Maleimidopropionoic acid is bound to the peptide via lysine which binds the free thiol of cycsteine-34 in albumin. The binding of the peptide in albumin creates a much longer and sustained effect of the drug. Due to this technology the half-life of CJC-1295 is 8-10 days in humans. (1,2,3)
CJC-1295 causes significant increases GH and IGF-1 so it will provide the same benefits found with the use of these growth factors. Healthy adults deficient in Growth Hormone can benefit in the following ways:
· increased exercise capacity
· increased muscle mass
· increased bone density
· decreased body fat
CJC-1295 Side Effects
CJC-1295 has been tested in humans with relative safety and effectiveness. S. Teichman et. Al conducted two randomized, double-blind, placebo-controlled studies. 66 Healthy adults, 21-64 years of age were administered subcutaneous CJC-1295. The peptide was dosed at 30-125 ug/kg of bodyweight, 1-3 times weekly or bi-weekly, for 28 and 49 days. The compound was most well tolerated at 30-60 μg/kg of bodyweight. There were no serious adverse events reported, most common side effect was injection site irritation. Other side effects included headache, diarrhea, and vasodilation. The study found a dose dependent increase in GH and IGF-1 levels. GH was increased 125% and IGF-1 was increased 80% for up to 6 days by just one single injection! M. Lonescu et. al assessed GH pulsatility of 20 healthy men ages 20-34 after a single injection of CJC-1295. Researches found a 40% increase in GH as opposed to an expected 75% increase, with no significant difference being found between a 60 μg/kg and 90 μg/kg doses. The natural GH pulsatility was maintained which dispels the “GH bleed” myth commonly mentioned in reference to this compound. This study found “no serious adverse effects,” most common side effects were increase in heart rate and injection site irritation. All side effects were short in duration.
During ConjuChem’s Phase II clinical trial of 192 subjects, a patient receiving their second to last CJC injection of the trial complained of chest pains two hours after injection. The patient underwent a ECG which identified a myocardial infarction, death occurred one hour later. ConjuChem’s states as follows:
“There is no evidence of any cardiotoxic effects of DAC(TM):GRF in previous preclinical or clinical studies. The attending physician stated that his most likely explanation for the event was the patient had asymptomatic coronary artery disease with plaque rupture and occlusion.”
CJC-1295 vs HGH
CJC-1295 has several advantages over exogenous HGH application. The most profound benefit is that CJC only requires administration once per week, this makes ease of use much greater. CJC stimulates natural release of GH and maintains the natural pulsatory nature of GH release in the body. This may reduce or avoid the common side effects associated with HGH use. Although this suggests CJC-1295 would be a better choice than HGH, I do believe that an athlete like a pro bodybuilder seeking a super human physique may be able to elevate GH and IGF-1 much higher with exogenous HGH. However, these levels may be able to be duplicated with the stacking of CJC along with other peptides.
CJC-1295 is commonly used in bodybuilding, fat loss, and life extension circles. Most conversation about and anecdotal accounts of CJC use take place on bodybuilding forums. This compound has not been approved by the FDA , therefore it is important to note that safety and dose have not been established for human use. CJC-1295 dose has been reported in a range of 0.1-10mg per week. The average reported doses seem to start at around 2mg with users ramping up to 6-8mg. The clinical research I cited used 30-125 μg/kg, this translates to 6-25 mg per week in a 200 lb person. These doses were well tolerated with little difference in results above 60 μg/kg.
CJC-1295 Doping and Detection
The detection of CJC-1295 administration has been shown in animal models via immunoassay methods. I was unable to find any accounts of qualitative detection in human competitive athletes. The reports of CJC-1295 use in sport have seemingly been accusations or evidential. However, there are reports of positive secretagogue PED tests for Ibutamoren, Ipamorelin, GHRP-6, and GHRP-2. (7,8)
CJC-1295 is readily available to purchase for research purposes. Optimized Peptides is a company I have used and trust. I like Optimized Peptides because they third party analyze each individual lot of product and they even supply the spectral data from the analysis. CJC-1295 is available directly from this link.
Optimized Peptides Coupon Code
You can support Radical Research by using our coupon code RR10 at checkout to receive a 10% discount on your purchase at Optimized Peptides!
1. Lucie Jetté, et al. July 2005. Human Growth Hormone-Releasing Factor (hGRF)1–29-Albumin Bioconjugates Activate the GRF Receptor on the Anterior Pituitary in Rats: Identification of CJC-1295 as a Long-Lasting GRF Analog. Endocrinology. Volume 146 (Issue 7). https://doi.org/10.1210/en.2004-1286
2. Maria Alba, et al. December 2006. Once-daily administration of CJC-1295, a long-acting growth hormone-releasing hormone (GHRH) analog, normalizes growth in the GHRH knockout mouse. APS Endocrinology and Metabolism. Volume 291 (Issue 6). https://doi.org/10.1152/ajpendo.00201.2006
4. Sam L. Teichman, et al. March 2006. Prolonged Stimulation of Growth Hormone (GH) and Insulin-Like Growth Factor I Secretion by CJC-1295, a Long-Acting Analog of GH-Releasing Hormone, in Healthy Adults. The Journal of Clinical Endocrinology & Metabolism. Volume 91 (Issue 3)
5. Madalina Lonescu, et al. December 2006. Pulsatile Secretion of Growth Hormone (GH) Persists during Continuous Stimulation by CJC-1295, a Long-Acting GH-Releasing Hormone Analog. The Journal of Clinical Endocrinology & Metabolism. Volume 91 (Issue 12)
N-Acetylserotonin: the grand child of 5-hydroxytryptophan and parent to melatonin.
N-Acetylserotonin is a melatonin precursor and downstream metabolite of 5-HTP. Melatonin, also known as N-acetyl-5-methoxy tryptamine, is a hormone produced in the pineal gland of animals which is involved in the regulation of circadian rhythms and also acts as an anti-oxidant. 5-Hydroxytryptophan, AKA Oxitripan AKA 5-HTP, is a naturally occurring precursor to serotonin. 5-HTP is produced by the enzyme tryptophan hydroxylase acting upon the amino acid tryptophan, 5-HTP is then decarboxylated to the neuro transmitter serotonin by the enzyme aromatic L-amino acid decarboxylase. The compound of interest N-acetylserotonin (NAS)is also referred to as Normelatonin; the illustration shows that NAS has structural similarities to both Melatonin and 5-HTP. It is an agonist of melatonin receptors MT1, MT2, and MT3. NAS shares some of melatonin's anti-oxidant effects but excels with greater anti-oxidant capacity, possible cognition enhancement, anti-aging, neuroprotective, antidepressant, and BDNF effects. (2)
N-Acetylserotonin is a naturally occurring chemical which is a precursor to melatonin in the pineal gland and retina. N-acetylserotonin is also present in the hippocampus, olfactory bulb, spinal cord and cerebellum. NAS is biosynthesized from serotonin by the enzyme arylalkylamine N-acetyltransferase. N-Acetylserotonin is not solely a precursor to melatonin, it exhibits bioactive properties independently and even targets areas of the brain that serotonin and melatonin do not.(4)(5) NAS was shown to perform better than melatonin in scavenging reactive oxygen species and far surpassed melatonin in protecting against radical-induced cell death.(1)(2) This tells us that NAS is a better antioxidant than melatonin.
N-Acetylserotonin serotonin levels were shown to increase in female Fisher 344N rats with the administration of the drug deprenyl at .25mg/kg. Deprenyl has been shown to increase life span and it has been suggested that NAS is the mechanism for life extension. NAS was administered to mice at 2.5mg/kg of bodyweight starting at four weeks of age, this extended the life of male C3H mice by more than 20%. This data suggests there may be anti-aging or life extension benefits from the exogenous administration or indirect increase of NAS due to NAS modulating drug administration. (11)
N-acetylserotonin has been shown to be an agonist of TrkB which is the same receptor brain-derived neurotrophic factor (BDNF) activates. (3)(9) It has also been suggested that NAS protects against B-amyloid toxicity which is associated with Alzheimer’s disease. It is also protective against MPP+ which is a drug with the ability to induce Parkinson’s disease. Additionally, NAS stimulates neuroprogenitor cells and prevents negative effects of sleep deprivation. (5)(8) N-Acetylserotonin levels have been shown to increase up to 5-fold with administration clorgyline, an irreversible and selective MAO-A inhibitor with antidepressive effects.(4)(10) As previously mentioned NAS activates TrkB, this is a trait that is shared with SSRIs, SNRIs, and clorgyline. Exogenous administration of NAS in mice shows a decrease of immobility in mouse tail suspension test. (4) These findings suggest that NAS has antidepressant properties, it has been postulated that increased levels of NAS induced by anti-depressant compounds may be responsible for the positive effects of these drugs. These findings may show that NAS is neuroprotective, cognition enhancing, and antidepressant. (5)(8)(9)
NAS exhibits a more diverse and potentially greater beneficial effects than both 5-HTP and Melatonin. NAS’s similarity in structure to 5-HTP and melatonin along with its biological roll as a precursor to melatonin make it a viable compound for a new dietary ingredient in OTC nutritional supplements.
1. N-acetylserotonin is a better extra- and intracellular antioxidant than melatonin; Albert Wölfler-1999
2.Antioxidant and Antiaging Activity of N-Acetylserotonin and Melatonin in the in Vivo Models; G. OXENKRUG-2001
3.N-acetylserotonin activates TrkB receptor in a circadian rhythml; Sung-Wuk Jang-2010
4.The effect of nifedipine, Ca2+ antagonist, on activity of MAO inhibitors, N-acetylserotonin and melatonin in the mouse tail suspension test; Irine V. Prakhie
5.N-Acetylserotonin Neuroprotection, Neurogenesis, and the Sleepy Brain; Gianluca Tosini
6. N-Acetylserotonin in the central nervous system; Gregory M.Brown
7. The serotonin-N-acetylserotonin–melatonin pathway as a biomarker for autism spectrum disorders; C Pagan
8. N-acetylserotonin promotes hippocampal neuroprogenitor cell proliferation in sleep-deprived mice; Pradoldej Sompol, Xia Liu- 2011
9. N-Acetylserotonin: Circadian Activation of the BDNF Receptor and Neuroprotection in the Retina and Brain; P. Michael- 2014
10. The effect of MAO-A inhibition and cold-immobilization stress on N-acetylserotonin and melatonin in SHR and WKY rats; G. F. Oxenkrug
11. N-Acetylserotonin and Aging-Associated Cognitive Impairment and Depression; Gregory Oxenkrug-2012
God is that you? No, it’s just the drugs.
Religion is no stranger to drugs, whether it is ethanol in Christianity dating back to AD33, Ayahuasca in the Santo Daime religion dating back to the 1930s, or the current administration of psilocybin to Religious leaders by Johns Hopkins University. There is no shortage of religious ceremonies, which permit the choice to partake in a chemically induced spiritual journey. However, if you have been to a religious ceremony in the past 4000 years you may have consumed a psychoactive substance without even knowing it!
Incensole acetate (IA) is the substance in mention. IA is a macrocyclic diterpenoid, which is the major bioactive constituent found in the resin of trees in the Boswellia species. The Boswellia species has been mentioned in many ancient texts as incense or a main component thereof. It is commonly referred to as frankincense or olibanum. Research by Dr. Arieh Moussaieff has shown incensole acetate to exhibit anti-depressive, anxiolytic, anti-inflammatory, and neuroprotective effects.
Incensole acetate displays anti-depressant and anxiolytic effects. It is always interesting to find a naturally occurring compound with a long history of use that exhibits positive psychoactive effects. Perhaps the most interesting aspect is the pathway which IA acts on. Researchers found no anti-depressive or anxiolytic effect in mice that lacked the transient receptor potential vanilloid 3 (TRPV3) gene. This allowed for the conclusion that IA elicits its psychoactive effects via TRVP3. TRVP3 is expressed in the skin and in the brain; its most well know function is temperature sensation and its two lesser understood functions are hair growth and mood regulation. IA was also found to have a “robust anti-inflammatory effect” when tested in mice with inflamed paw model.
Incensole Acetate also exhibits many neurological benefits. It has been shown to inhibit hippocampal neurodegeneration. IA was also shown to reduce severity of head injury; in a mouse model of closed head injury, mice showed reduced neurological severity scores and improved cognitive ability. Later research by Dr. Mousaieff shows a decrease in corticotropin releasing factor and up regulation of brain derived neurotrophic factor (BDNF). This suggests a possible effect on the hypothalamus-pituitary-adrenal axis.
The extract of Boswellia serrata gum resin, standardized to 65% organic acids, is currently available through online nutritional supplement vendors. It is available in capsule and liquid forms. The amount of incensole acetate provided from these supplements is unknown. It would be great to see a purified or synthesized version of incensole acetate available as a supplement, nootropic, or “research chemical.”
There is no doubt the work of Dr. Moussaieff has brought the many benefits of this compound to the attention of the scientific community. The information is now in our hands and it will be beneficial to promote interest in this compound.
1. Arieh Moussaieff , Et al. May 2008. Incensole acetate, an incense component, elicits psychoactivity by activating TRPV3 channels in the brain. The Faseb Journal. Vol. 22 #8.
2. Arieh Moussaieff , Et al. December 2007. Incensole Acetate, a Novel Anti-Inflammatory Compound Isolated from Boswellia Resin, Inhibits Nuclear Factor-κB Activation. Molecular Pharmacology. Volume 72 Issue 6.
3. Arieh Moussaieff , Et al. April 2018. Incensole Acetate: A Novel Neuroprotective Agent Isolated from Boswellia Carterii. Journal of Cerebral Blood Flow and Metabolism. Volume 28 Issue 7.
Vincamine is monoterpenoid indole alkaloid with peripheral vasodilation properties. It is a naturally occurring alkaloid found in the leaves of Vinca minor or lesser periwinkle. Vincamine could be referred to as the “natural version” of vinpocetine; with vinpocetine being a synthetic ethyl ester version of vincamine. In 2016 the FDA announced that vinpocetine does not meet the definition of a dietary ingredient and is therefore illegal for use in dietary supplements. FDA states that in 1981 vinpocetine was subject of an Investigational New Drug (IND) application. According to federal law, compounds that have had IND filing can’t later submitted for New Dietary Ingredient (NDI). Conversely compounds that have been marketed as dietary supplements can be developed into a drug. Vincamine’s close similarity in structure and function when compared to vinpocetine makes it a viable replacement compound for vinpocetine containing supplements.
Vincamine is a peripheral vasodilator, therefore increase blood flow to the brain. Vincamine exhibits positive neuropharmacological effects which make it an attractive nootropic compound. ( Hagstadius et al. 1984) observed significant increases in global cerebral blood flow, performance on verbal memory test, and decrease in ischemic regions. In a 12 week double blind placebo; 30mg twice daily was superior to placebo for treatment of patients with mild to moderate dementia of degenerative and vascular etiologies (Fischhof et al. 1996). Vincamine was also found to increase the firing rate of neurons in the locus coeruleus of rat brains (Olpe 1982). The locus coeruleus is related to many functions including: arousal, sleep-wake cycle, attention, memory, behavioral flexibility, stress, cognitive control, emotions, neuroplasticity, posture, and balance. Interesting side note, according to (Schwartz et al. 2008) neurons in the locus coeruleus cease firing during REM sleep. There is also a patent from 1979 which claims the salt of vincamine pyridoxal-5-phosphate exhibits greater activity than vincamine alone along with anti-depressive effects.
I have yet to see vincamine sold as a supplement or nootropic powder. However, it can be found in 30mg time release capsules under the trade name Oxybral SR by GSK. This is sold in countries outside of the US.
I happened to come across @optimresearchinfo 's page and noticed a compound very near and dear to my heart, I had to have it! It is a 2-ene steroid, 17B-acetoxy-5a-androst-2-ene aka desoxytestosterone acetate. 2-ene steroids are so fantastic because they fly in the face of conventional structure activity relationship for anabolic androgenic steroids. Which would insinuate "you must have a 3-ketone and 17-hydroxyl group to bind the #androgenreceptor." 2-ene steroids lack the 3-keto group yet bind the androgen receptor with a very favorable ratio.
Let's dig into the rich history of these steroids. Patrick Arnold, who is touted with many unique and effective contributions to the performance enhancing industry, had reintroduced and synthesized desoxymethyltestosterone (DMT) for athletes. DMT was one of the coumpounds mentioned along side THG or tetrahydrogestrinone, in the ever so famous "BALCO scandal." Soon after this, DMT was widely sold and marketed as a "pro hormone" or "pro steroid" and sold openly in the nutritional supplement market. This compound eventually became noticed by authorities. Soon after, the same company that had marketed DMT as Pheraplex, Anabolic Xtreme, then released 3-AD which was the compound 17b-acetoxy-5a-androst-2-ene. This compound was the removal of 17a-methyl group from DMT and edition of an 17B-acetate group. This company then discontinued the product. Moving forward the now defunct company, ANDROGENETX, released Delta-2 which was 5a-androst-2-ene-17-one a precursor to 5a-androst-2-ene-17b-OH. This was sold as a supplement and is arguably DSHEA compliant due to the fact it is a human metabolite of DHEA and present in specific game meat such a wild boar. Delta-2 is still available to this day from @olympus_labs as Sup3r-2.
@optimresearchinfo has available 17B-acetoxy-5a-androst-2-ene in sterile oil. You can expect profound muscle and strength increase with minimal sides from this! .
AKA: gamma-Amino-beta-hydroxybutyric acid or 4-amino-3-hydroxybutanoic acid
GABOB is a lesser known metabolite and analogue of #GABA, which is available on the Internet under the trade name Gamibetal. It is sold as an anticonvulsant for epilepsy in Europe, Japan, and Mexico.
Structurally GABOB resembles GABA with a hydroxyl group at the 3 position.
GABOB functions as an inhibitory neurotransmitter, which produces anxiolytic and anticonvulsant effects. Studies have shown dose dependent effects of GABOB on #growthhormone levels, although I could not find any that used oral administration.
Users can expect effects similar to GABA but with greater potency; due to GABOB's ability to cross the blood-brain barrier. GABOB should make for an effective sleep/relaxation aid.
Please note 18 & 19 position carbons were not drawn.
Demalon aka 1a,17a-dimethyl-5-androstan-17-ol-3-one is a #steroid that to the best of my knowledge has never been released. You can see the resemblance to #methasterone which was commonly known as #superdrol and #metenolone aka #methenolone or #primobolan. This would be a potent and liver toxic oral #DHT derivative.
AKA: (-)-BPAP, -)-1-(Benzofuran-2-yl)-2-propylaminopentane, or BFPAP
BPAP is a drug that was developed for use in delaying the onset/development of Parkinson's and Alzheimer's, similar to #deprenyl or #selegiline. It is available via clear net vendors.
BPAP is unique as it is a catecholamine activity enhancer; acting upon #serotonin#norepinephrine and #dopamine. This means it enhances the release of these #neurotransmitters in response to stimuli, as opposed to just causing an uncontrolled release as with #cocaine and #molly. It also exhibits #neuroprotective properties.
BPAP is similar to (-)deprenyl however it is #tryptamine derived as opposed to #phenylethylamine derived. It is more potent catecholamine enhancer but is also a much weaker inhibitor of MAO-A when compared to (-)deprenyl.
This compound is Diosgenone which has been isolated from Solanum nudum and also has been synthesized. #diosgenone is a #diosgenin related steroidal sapogenin. Diosgenin along with many other #steroidal #saponins are included in #muscle #building #supplements for there purported #protein #synthesis enhancing properties. The most recent and popular has been #5ahydroxylaxogenin or #laxogenin. Diosgenone contains 4-ene and 3-one substituents which are present in testosterone and necessary for binding the #androgen receptor. Though Diosgenone lacks the 17-hydroxyl group necessary for androgen binding, it may still exhibit greater
3,4-methylenedioxy-n-methylphenylethylamine #mdmpea is similar to #mdma in that it contains 3,4-methylenedioxyphenylethylamine #mdpeahowever the #methyl group is located at the #nterminus as opposed to the alpha position. MDMPEA will exhibit #enactogen#psychedelic and #stimulant properties. However, the effective dose may be very large or effects short lived; due to #firstpassmetabolism #monoamineoxidase. Metabolism may be similar to MDPEA which #alexandershulgin deemed inactive. The n-methyl group may provide some protection against #mao. Regardless this would be an interesting compound to #research.
Mangiferan is a truly awesome #chemical. It is a naturally occurring xanthonoid that is a #polyphenolof c-glycosylxanthone.
Mangiferan caught my interest because of its #maoi #memoryenhancing and #neuroprotective properties.
According to Matkowski A, et al. it exhibits analgesic, antidiabetic, antisclerotic, antimicrobial and antiviral, cardio-, hepato-, and neuroprotective, antiinflamatory, antiallergic, and radioprotective properties.
Mangiferan is found in many plant species including mango. Therefore it would be a viable option for a legal #researchchemicalor #dshea compliant #supplement.
3β-Hydroxy-1,4-androstadien-17-one undecanoate (pictured in 1) is a new #prohormone that
was recently released by @hitechpharma as #equibolan. This compound is #Androsterone with a double bond located at the 1 and 4 position of the A ring and an undecanoate ester located at the 3b-hydroxy group. It could also be referred to as 1,4-DHEA with the esterfied 3 hydroxyl group. This compound is a precursor to #boldione (pictured in 2) and #boldiol(same as Boldione but with -OH groups at 3 and 17 instead of the =O) with both of those compounds being metabolized to #boldenone (pictured in 3) it is ultimately a prohormone to Boldenone. The undecanoate ester makes the compound more #lipophilic which enhances absorption when consumed with a fat containing meal. This helps to deliver the compound via the lymphatic system as opposed to being subject to initial destruction by #firstpassmetabolism in the liver. You can most likely expect very mild results with similarities to Boldenone. I would probably dose this compound higher than the directions recommend. However, I can't be sure as I have not tried it yet.
Mesembrine is one of the prominent #alkaloids present in Sceletium tortuosum aka #kanna #mesembrineexhibits #ssri and #pde4 inhibiting properties. The benefits of Mesembrine are enhanced mood, decreased anxiety, procognitive, wakefulness promoting, anti-inflammatory effects. This alkaloid and/or the kanna extract make for a #nootropicand #moodenhancing #researchchemicalor #supplement Sceletium tortuosum extract can be found in #psychopreworkoutby @scivation #c4neuro by @cellucor and #noopump by @mansports
Withanolides are naturally occurring C28 steroidal lactones. There have been over 300 #steroids identified and they are common in various solanaceous #plants. Most notably in Withania somnifera AKA #ashwagandhaExtracts of these plants have been used in #ayurvedic #unani and #chinesemedicine. Withanolides harness a plethora of benefits including #nootropic #adaptogenic#antioxidant #antistress#immunomodulating #antiinflamatory#antimicrobial #antitumor and #hepatoprotective. Withanolides and a very exciting #steroid in that they have many uses for #drugs #researchchemicals and #supplements
Hyperforin is a naturally occurring phytochemical. It is most notably found in Hypericum perforatum which is more commonly known as St. John's wort. Hyperforin is believed to be the main constituent attributed to the #anxiolyticand #antidepressant effect of #stjohnswort. Hyperforin produces anxiolytic effects via reuptake inhibition of #gaba and #nmdareceptor modulation. The antidepressant or #moodboosting effects are due to MAO-A and MAO-B inhibition along with the inhibition of #norepinephrine, #serotonin, and #dopamine reuptake. Hyperforin has also shown #nootropic capabilities by inhibiting reuptake of #glycine and #choline as well as modulating #acetylcholine.
AKA: Oxilofrine, hydroxyephrine, oxyephrine, and 4-HMP.
News: FDA has determined this is not a dietary ingredient after years of use.
This compound is #synephrine with a #methyl group attached to the alpha carbon.
#Methylsynephrine will have similar effects to synephrine. However, the half life will most likely be close to double that of synephrine. That is due to the #sterichinderance of the methyl group preventing #drug destruction via #mao or #monoamineoxidase.
#Oxilofrine activates beta adrenergic receptors. It is preferential to Beta 2 & 3, over beta 1. This is preferential for #performanceenhancingdrugs because beta-2 #adrenergic receptor will promote vasodilation in skeletal muscle and beta-3 will promote #fatloss.
Oxilofrine is a very mild central nervous system #stimulant due to the beta-hydroxyl group which prevents blood-brain-barrier permeability.
MDHR™ (Methyl-Dihydrorubrosterone) is a novel #steroid compound available exclusively from @alr_industries as Pro Anabol. I believe it is 17-methylated Dihydrorubrosterone which is a naturally occurring plant sterol that has been isolated Silene otites.
The most interesting and exciting thing about this compound is that it contain a 17-hydroxyl group which is necessary for androgen receptor binding. It also contains a 3-hydroxyl group which can be converted in vivo by 3beta-Hydroxysteroid dehydrogenase (3b-HSD) in to a 3-Keto group which is also necessary for androgen binding. There is also a ketone at the 6 position which will cause the steroid to exhibit some aromatase inhibition capability; as seen with the #drugexemestane and 6-OXO or androstenetrione which was previously sold as a #supplement. However, I would guess that the aromatase inhibiting activity would be mild as #exemestane derivatives are 3-8 times less potent aromatase inhibitors when there is a hydroxyl group at the 17 position.
The 17-hydroxyl group on MDHR is protected from liver destruction by the addition of a #methyl group, known as 17-alpha alkylation.
ALRI claims that there is zero liver toxicity. However, if this compound is in fact 17-alpha alkylated I can only assume there would be some liver toxicity.
isomerdesign.com lists this compound as having a 17-methoxy group. If that is the case the 17-methoxy group would actually decrease androgen activity and increase progestin activity.
Tesofensine is a very interesting compound. It is a phenyltropane with #serotonin #norepinephrine #dopaminereuptake inhibiting properties and potentiates cholinergic neurotransmission. NS2330 has #antidepressant, #weightloss, and #nootropic properties.
Tesofensine was initially in development for #alzheimers and #parkinsons treatment. The drug was abandoned for these treatments however weight loss was a side effect noted in trials. The drug is now under development for treating obesity in Mexico and Argentina.
Etifoxine is an #unregulated #anxiolytic and anticonvulsant #drug that was developed for #anxiety disorders in the 1960's. It is currently being investigated for peripheral nerve healing and #chemotherapy induced #pain.
Etifoxine has similar effects to #benzodiazepines with little to no withdrawal effects. It is mediated by GABAAα2 and binds directly β2 or β3 subunits of the GABAA. Etifoxine has a relative high oral bioavailability and a standard dose of 150mg per day for no more than 12 weeks.
AKA: Marsilid, Rivivol, Euphozid, Iprazid, Ipronid, Ipronin
Iproniazid is a non-selective, irreversible, monoamine oxidase inhibitor #maoi.
Iproniazid initially caught my attention due to its distant similarity to #cathinone. Surprisingly, the most interesting aspect of iproniazid is its history as opposed to its pharmacology.
The year was 1951; Isomiazid and Iproniazid, two hydrazide derivatives, were introduced for the treatment of tuberculosis by Roche, Squibb, and Lily. Soon after Iproniazid's introduction, Nathan Kline discovers its #antidepressant effects. Jack Saunders, a former employee of Ciba, then joins Kline at Rockland State Hospital of #NewYork in 1956 to study the #psychotropic effects of Iproniazid. In 1957 Kline believed the drugs antidepressant effects were significant and approached the managing director of Roche, David Barney. However, Barney showed little interest in the Iproniazid. Later in the year Kline went on to present the "Psychic Energizing" effects of Iproniazid at the American Psychiatric Association's regional meeting in #Syracuse, New York. This presentation was reported by the #NewYorkTimes and soon after Iproniazid was being used for "anti nervousness properties." This discovery earned Kline the Lasker Award, and he was invited to write and article on Iproniazid in the Journal of American Medical Association. Later on Kline's former partner Saunders sued for a portion of the Lasker prize. There were several hearings prior to Kline's death in 1981. However, it has been said that previous research of Max Lurie trumps both Kline's and Saunders'. Source: History of Psychiatry and Medical Psychology
NS9775 is compound that is both a monoamine reuptake inhibitor (MRI) and a7 nicotinic #acetylcholinereceptor (nAChR) agonist. MRIs are typically used in the treatment of depression or #ADHD due to their ability to increase the availability of #monoamine#neurotransmitters. MRIs promote increased levels of #serotonin, #norepinephrine, and #dopamine. nAChR agonists promote cognitive function and facilitate monoamine release. MRIs and nAChR agonist have been shown to work in synergy against depression.
Though there is a lack of any human data, clinical or anecdotal; there have been behavioral effects shown in mice studies.
Mice displayed reversed scopolamine-induced deficits, increased forced swim distance, reduced digging in marble burying paradigm, and increased number of punished plate crossings.
This is a very interesting compound that displays pro-cognitive, #antidepressant, and #anxiolytic effects. It is surprising that it has not surfaced in #nootropic or #researchchemical communities yet.
Amiflamine is an unregulated #phenylethylamine / #amphetamine derivative that seemed to have some light research in the 80's. It is a reversible MAO-A inhibitor. It also shows evidence that it is a #catecholaminereleasing agent.
The rodent model displayed a preference to MAOI in the serotonergic neurons. The primate model used cerebral spinal fluid (CSF) markers to suggest the compound acts equally on #serotonin #norepinephrineand #dopamine metabolism. However, the same primate study showed a preference to serotonin and dopamine at lower doses. There were minimal amounts of Amiflamine and larger amounts of two bioactive metabolites found in CSF after 3-6 hours.
There was actually a human study run with 9 inpatients. This obviously did not provide any statistically significant conclusions. However, I will note that the patients did receive 2.5-5mgs twice per day for three weeks. The most noted side effects were trouble sleeping and headaches. .
B-Carboline and it's derivatives are naturally occurring plant #alkaloids. They harness some fairly potent #psychoactive effects via MAOI, acetylcholinesterase inhibition, and inverse #benzodiazepine agonism. Some derivatives may exhibit #neurotoxicity , however some synthetic analogues have been shown to be #neuroprotective. #harmine , #harmaline , and tetrahydroharmine are commonly found in #peganumharmala and #banisteriopsiscaapi. These plants are used in ayahuasca brews to prevent destruction of #DMT by monoamine oxidase.