Α-Methylserotonin Explained

α-Methylserotonin (αMS), also known as α-methyl-5-hydroxytryptamine (α-methyl-5-HT) or 5-hydroxy-α-methyltryptamine (5-HO-αMT), is a tryptamine derivative closely related to the neurotransmitter serotonin (5-HT). It acts as a non-selective serotonin receptor agonist and has been used extensively in scientific research to study the function of the serotonin system.[1]

Unlike serotonin, αMS is not metabolized by monoamine oxidase on account of the α-methyl substituent blocking the enzyme's access to the amine. As a result, it has a much longer half-life in comparison.[2] [3] Similarly to serotonin however, αMS poorly crosses the blood-brain-barrier due to its free hydroxyl group, and thus has only weak or no central effects when administered peripherally.[2]

α-Methyltryptophan (αMTP) is a prodrug to αMS which does cross the blood-brain-barrier and thus efficiently delivers αMS into the central nervous system.[4] [5] As a result, αMTP acts as an orally bioavailable false or substitute neurotransmitter for serotonin, and has been suggested as a possible therapeutic agent in the treatment of disorders where serotonin is deficient.[4] [5] The O-methylated analogue of αMS, 5-MeO-αMT, also readily enters the brain and could be used for this purpose as well.[2] [6]

Legal status

United States

5-Hydroxy-alpha-methyltryptamine is not scheduled at the federal level in the United States,[7] but it could be considered an analog of alpha-methyltryptamine (AMT), in which case, purchase, sales, or possession could be prosecuted under the Federal Analog Act.

Florida

5-Hydroxy-alpha-methyltryptamine is a Schedule I controlled substance in the state of Florida making it illegal to buy, sell, or possess in Florida.[8]

See also

Notes and References

  1. Ismaiel AM, Titeler M, Miller KJ, Smith TS, Glennon RA . 5-HT1 and 5-HT2 binding profiles of the serotonergic agents alpha-methylserotonin and 2-methylserotonin . Journal of Medicinal Chemistry . 33 . 2 . 755–8 . February 1990 . 2299641 . 10.1021/jm00164a046.
  2. Web site: Erowid Online Books : "TIHKAL" - #48 a-MT .
  3. Diksic M, Nagahiro S, Sourkes TL, Yamamoto YL . A new method to measure brain serotonin synthesis in vivo. I. Theory and basic data for a biological model . Journal of Cerebral Blood Flow and Metabolism. 10 . 1 . 1–12 . January 1990 . 2298826 . 10.1038/jcbfm.1990.2. free .
  4. Sourkes TL, Montine TJ, Missala K . Alpha-methylserotonin, a substitute transmitter for serotonergic neurons . Progress in Neuro-psychopharmacology & Biological Psychiatry . 14 . 5 . 829–32 . 1990 . 1705718 . 10.1016/0278-5846(90)90055-l. 25604266 .
  5. Sourkes TL . Alpha-methyltryptophan as a therapeutic agent . Progress in Neuro-psychopharmacology & Biological Psychiatry . 15 . 6 . 935–8 . 1991 . 1763198 . 10.1016/0278-5846(91)90020-2. 31504647 .
  6. Web site: Erowid Online Books : "TIHKAL" - #5. a,O-DMS .
  7. Web site: §1308.11 Schedule I. . 2014-12-17 . 2009-08-27 . https://web.archive.org/web/20090827043725/http://www.deadiversion.usdoj.gov/21cfr/cfr/1308/1308_11.htm . dead .
  8. http://leg.state.fl.us/statutes/index.cfm?App_mode=Display_Statute&URL=0800-0899/0893/0893.html Florida Statutes - Chapter 893 - DRUG ABUSE PREVENTION AND CONTROL