DOSE:

sublingual

Pinoline

(powder / crystals)

BODY WEIGHT:

80 kg

Human bioassay of Pinoline

6-Methoxy-1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indole; 6-Methoxy-1,2,3,4-tetrahydro-β-carboline; 6-MeO-THBC.

Given the complete lack of human reports for pinoline, some was acquired and bioassayed, this being an endogenous compound MAOI compound that could be interesting and certainly worthy of looking at by someone. Despite its name, solid evidence that pinoline is made in the human pineal gland is lacking. Research has indicated that pinoline passes the blood brain barrier poorly[1] and inhibits MAOI with an IC50 of 1.6um, which is around 1,000 less potent than harmine, and that you need a good 100mg/Kg in rodents to exceed 50% MAO inhibition[2]. Still it was worth checking for psychoactivity outside of its MOAI effect. A special thanks to my Nexian friend who helped facilitate this.

500 mg of pinoline (97% purity) was obtained from a well-known chemical supply company and bioassayed at various dosages (10 mg, 50 mg, 2x 100 mg, 200 mg). Samples were weighed via balance sensitive to 0.0001 g. All doses were ingested sublingually, under the tongue, unless otherwise stated, following brushing of teeth and gums. Dose was held for 20 minutes under tongue before swallowing. All doses were consumed in the late evening (after 10PM) in subject’s bedroom, with the only ambient light being candle light (not found to repress melatonin production, a precaution in case a similar mechanism applies to pinoline). Subject was sober on all days of experiments with no other substances in system. Body weight of subject is 80 kg. Subject has previous experience (including sublingual use) of related compounds such as melatonin and plant derived beta-carbolines.

10 mg. (0.13mg/Kg). Slight feeling of relaxation and sedation. Very subtle, could be placebo.

50 mg. (0.63mg/Kg). 15 minutes after dosing, a feeling of relaxation and slight sedation felt. Sleep following experiment was deep and restful.

100 mg. (1.25mg/Kg). Dose insufflated. Subject immediately regretted this route of administration, due to intense nasal burn, and decided to abort experiment. After pain died down a feeling of relaxation experienced but could be partly down to influence of endorphins.

100 mg. (1.25mg/Kg). 10/15 minutes after dosing, a feeling of relaxation and slight sedation washes over subject. Feeling is reminiscent of a large dose of melatonin, with just a pinch of harmaline, although lacking the visionary psychoactive effects of the latter. Deep sleep following experiment.

200 mg. (2.5mg/Kg). 10/15 minutes after dosing, a feeling of calm relaxation and slight sedation washes over subject. Seemingly little difference between this and the 100 mg dose in effect. No other noticeable effects noted.

Comments

At these dosages and via this route of administration, pinoline produced definite but subtle effects, primarily experienced as a feeling of calm and relaxation, a slight sedation and increased desire to lie down and relax. Feeling is most reminiscent of a large dose of melatonin, although did not seem to affect dreams like the latter can. Compared to 250 mg of pure (98%) harmaline hcl, the latter was experienced as a great deal more psychoactive in comparison, producing many more mental and physical effects, at this level pinoline was only slightly physical in effect. Pinoline was well tolerated at these dosage levels, no trace of side effects or hangover were experienced.

At these dosages via this route of administration, pinoline had much more in common with the effects profile of melatonin than the plant derived beta-carbolines. So nothing Earth-shattering here, but I guess any result is a step forward!

I know myself and others have experienced a mild harmalaesque visionary head space having ingested supplemental melatonin and woken during the night. While pinoline may be much more potent when produced in situ in the brain on the right sound of the blood brain barrier, I'm now not so sure pinoline is responsible for these mild psychedelic effects experienced by myself and others. The pineal metabolises melatonin into other compounds such as 5-Methoxytryptamine (aka Mexamine) and this be partly responsible for such effects.


References

1. Leino, M., Airaksinen, M.M., Antikainen, R., Gynther, J., Kari, E., Kari, I. & Peura P. (1984) Distribution of 1,2,3,4-tetrahydro-beta-carboline and 6-methoxy-1,2,3,4-tetrahydro-beta-carboline in mice. Acta Pharmacologica et Toxicologica, 54, (5), 361-371.

2. Sparks, D.L., Buckholtz, N.S. (1980) 6-Methoxy-1,2,3,4-tetrahydro-beta-carboline: a specific monoamine oxidase-A inhibitor in CF-1 mouse brain. Neuroscience Letters, 20, (1), 73-8.

Exp Year: 2015	ExpID: 107120
Gender: Male
Age at time of experience: 30
Published: Oct 20, 2015	Views: 4,272
[ View PDF (to print) ] [ View LaTeX (for geeks) ] [ Swap Dark/Light ]
Pinoline (718) : First Times (2), Retrospective / Summary (11), Unknown Context (20)