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LY-301317

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LY-301317
Clinical data
Other namesLY301317; (R)-4,α-Methylene-5-(1,3-oxazol-5-yl)-N,N-dipropyltryptamine; (R)-4,α-Methylene-5-(1,3-oxazol-5-yl)-DPT
Drug classSerotonin 5-HT1A receptor agonist; Simplified/partial LSD analogue
ATC code
  • None
Identifiers
  • (4R)-6-(1,3-oxazol-5-yl)-N,N-dipropyl-1,3,4,5-tetrahydrobenzo[cd]indol-4-amine
PubChem CID
ChemSpider
Chemical and physical data
FormulaC20H25N3O
Molar mass323.440 g·mol−1
3D model (JSmol)
  • CCCN(CCC)[C@H]1CC2=CNC3=C2C(=C(C=C3)C4=CN=CO4)C1
  • InChI=1S/C20H25N3O/c1-3-7-23(8-4-2)15-9-14-11-22-18-6-5-16(17(10-15)20(14)18)19-12-21-13-24-19/h5-6,11-13,15,22H,3-4,7-10H2,1-2H3/t15-/m0/s1
  • Key:WVWRMVCFJMZWKO-HNNXBMFYSA-N

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

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References

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  1. ^ a b c Gaster LM, King FD (1998). "Latest Developments in Serotonin Receptor Modulation". Annual Reports in Medicinal Chemistry. Vol. 33. Elsevier. 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. ^ a b c d e Wolff MC, Benvenga MJ, Calligaro DO, Fuller RW, Gidda JS, Hemrick-Luecke S, et al. (1997). "Pharmacological profile of LY301317, a potent and selective 5-HT1A agonist". Drug Development Research. 40 (1): 17–34. doi:10.1002/(SICI)1098-2299(199701)40:1<17::AID-DDR2>3.0.CO;2-W. ISSN 0272-4391.
  3. ^ Wolff MC, Leander JD (August 1997). "Differentiation of 5-HT1A receptor ligands by drug discrimination". European Journal of Pharmacology. 333 (2–3): 113–122. doi:10.1016/s0014-2999(97)01125-4. PMID 9314023.
  4. ^ Andrews PL (1999). "Postoperative Nausea and Vomiting". Problems of the Gastrointestinal Tract in Anesthesia, the Perioperative Period, and Intensive Care. Berlin, Heidelberg: Springer Berlin Heidelberg. pp. 267–288. doi:10.1007/978-3-642-60200-9_31. ISBN 978-3-642-64301-9.
  5. ^ Leander JD (1996). "Behavior-enhancing effects of 5HT1A agonists and 5HT2 antagonists on a Progressive Ratio schedule". European Neuropsychopharmacology. 6: 52. doi:10.1016/0924-977X(96)87542-0.
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