|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||395.547 g·mol−1|
|3D model (JSmol)|
|(what is this?)|
WAY-100135 is a serotonergic drug of the phenylpiperazine family which is used in scientific research. It acts as potent 5-HT1A receptor antagonist, and was originally believed to be highly selective, but further studies have demonstrated that it also acts as a partial agonist of the 5-HT1D receptor (pKi = 7.58; virtually the same affinity for 5-HT1A), and to a much lesser extent, of the 5-HT1B receptor (pKi = 5.82). These findings may have prompted the development of the related compound WAY-100635, another purportedly selective and even more potent 5-HT1A antagonist, which was synthesized shortly thereafter. However, WAY-100635 turned out to be non-selective as well, having been shown to act additionally as a potent D4 receptor agonist later on.
- Fletcher A, Bill DJ, Bill SJ, et al. (June 1993). "WAY100135: a novel, selective antagonist at presynaptic and postsynaptic 5-HT1A receptors". European Journal of Pharmacology. 237 (2–3): 283–91. doi:10.1016/0014-2999(93)90280-u. PMID 8365456.
- Cliffe IA, Brightwell CI, Fletcher A, et al. (May 1993). "(S)-N-tert-butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide [(S)-WAY-100135]: a selective antagonist at presynaptic and postsynaptic 5-HT1A receptors". Journal of Medicinal Chemistry. 36 (10): 1509–10. doi:10.1021/jm00062a028. PMID 8496920.
- Davidson C, Ho M, Price GW, Jones BJ, Stamford JA (June 1997). "(+)-WAY 100135, a partial agonist, at native and recombinant 5-HT1B/1D receptors". British Journal of Pharmacology. 121 (4): 737–42. doi:10.1038/sj.bjp.0701197. PMC 1564750. PMID 9208142.
- Fornal CA, Metzler CW, Gallegos RA, Veasey SC, McCreary AC, Jacobs BL (August 1996). "WAY-100635, a potent and selective 5-hydroxytryptamine1A antagonist, increases serotonergic neuronal activity in behaving cats: comparison with (S)-WAY-100135". The Journal of Pharmacology and Experimental Therapeutics. 278 (2): 752–62. PMID 8768728.
- Chemel BR, Roth BL, Armbruster B, Watts VJ, Nichols DE (October 2006). "WAY-100635 is a potent dopamine D4 receptor agonist". Psychopharmacology. 188 (2): 244–51. doi:10.1007/s00213-006-0490-4. PMID 16915381. S2CID 24194034.