Chemistry:LY-301317

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LY-301317, also known as (R)-4,α-methylene-5-(1,3-oxazol-5-yl)-N,N-dipropyltryptamine ((R)-4,α-methylene-5-(1,3-oxazol-5-yl)-DPT), is a potent and selective serotonin 5-HT1A receptor agonist which has been used in scientific research.[1][2] It is a cyclized tryptamine and a partial ergoline.[2] The drug shows very high affinity for the serotonin 5-HT1A receptor, with a Ki of 0.26 nM, and is highly selective for this receptor over 9 other assessed targets.[1][2] It produces various serotonin 5-HT1A receptor agonist-associated effects in animals, including behavioral effects, hypothermia, antidepressant-like, anxiolytic-like, and antiemetic effects, and discriminative stimulus effects in drug discrimination tests.[1][2][3][4] LY-301317 was first described in the scientific literature in 1996.[5][2]

See also

References

  1. ↑ 1.0 1.1 1.2 "Latest Developments in Serotonin Receptor Modulation". Annual Reports in Medicinal Chemistry. 33. Elsevier. 1998. pp. 21–30. doi:10.1016/s0065-7743(08)61068-4. ISBN 978-0-12-040533-6. "Preclinical studies have continued with reports of more selective agents such as 1 (LY301317) which displaces [3H]-8-OH-DPAT binding to 5-HT1 A receptors in rat hippocampus with Ki of 0.26nM and shows > 200 fold selectivity over 9 other receptors tested. In vivo, 1 demonstrated 5-HT1A receptor agonist activity and was able to induce lower lip retraction and flat body posture in rats at 3mg/kg p.0. (22). In pidgeons and rats, 1 increased the rate of punished responding without affecting unpunished responding, indicative of a non-sedative anxiolytic profile. In the forced swim test in rats, 1 significantly decreased immobility time at 1 and 3 mg/kg S.C. in common with a number of antidepressants agents." 
  2. ↑ 2.0 2.1 2.2 2.3 2.4 "Pharmacological profile of LY301317, a potent and selective 5-HT1A agonist". Drug Development Research 40 (1): 17–34. 1997. doi:10.1002/(SICI)1098-2299(199701)40:1<17::AID-DDR2>3.0.CO;2-W. ISSN 0272-4391. 
  3. ↑ "Differentiation of 5-HT1A receptor ligands by drug discrimination". European Journal of Pharmacology 333 (2–3): 113–122. August 1997. doi:10.1016/s0014-2999(97)01125-4. PMID 9314023. 
  4. ↑ "Postoperative Nausea and Vomiting". Problems of the Gastrointestinal Tract in Anesthesia, the Perioperative Period, and Intensive Care. Berlin, Heidelberg: Springer Berlin Heidelberg. 1999. pp. 267–288. doi:10.1007/978-3-642-60200-9_31. ISBN 978-3-642-64301-9. 
  5. ↑ "Behavior-enhancing effects of 5HT1A agonists and 5HT2 antagonists on a Progressive Ratio schedule". European Neuropsychopharmacology 6: 52. 1996. doi:10.1016/0924-977X(96)87542-0. 


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