Chemistry:LY-293284

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LY-293284, also known as 4,α-methylene-5-acetyl-DPT, is a research chemical developed by the pharmaceutical company Eli Lilly and used for scientific studies. It acts as a potent and selective 5-HT1A receptor full agonist (Ki = 0.088 nM; EC50 = 0.13 nM).[1] It was derived through structural simplification of the ergoline based psychedelic LSD,[2] but is far more selective for 5-HT1A with over 1,000-fold selectivity over other serotonin receptor subtypes and other targets.[3] It has anxiogenic effects in animal studies.[4] In addition, it does not substitute for LSD in rodent drug discrimination tests.[1]

See also

References

  1. 1.0 1.1 "Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines". J Med Chem 43 (24): 4701–4710. November 2000. doi:10.1021/jm000339w. PMID 11101361. 
  2. "Substituted naphthofurans as hallucinogenic phenethylamine-ergoline hybrid molecules with unexpected muscarinic antagonist activity". Journal of Medicinal Chemistry 41 (12): 2134–45. June 1998. doi:10.1021/jm980076u. PMID 9622555. 
  3. "Pharmacological characterization of LY293284: A 5-HT1A receptor agonist with high potency and selectivity". The Journal of Pharmacology and Experimental Therapeutics 270 (3): 1270–81. September 1994. PMID 7523657. 
  4. "Comparative effects of novel 5-HT1A receptor ligands, LY293284, LY315712 and LY297996, on plus-maze anxiety in mice". Psychopharmacology 139 (3): 185–94. October 1998. doi:10.1007/s002130050703. PMID 9784072.