A 5-HT1A receptor antagonist
(S)-WAY 100135 dihydrochloride is a potent and selective antagonist of 5-HT1A receptor with IC50 value of 15 nM.
The 5-HT1A receptor is a G protein-coupled receptor for endogenous neurotransmitter serotonin (5-HT) and mediates inhibitory neurotransmission.
(S)-WAY 100135 dihydrochloride is a potent and selective somatodendritic and postsynaptic 5-HT1A receptors antagonist. (+/-)-WAY100135 inhibited 5-HT1A receptor in the rat hippocampal with IC50 value of 34 nM [1].
In the murine elevated plus-maze test, (S)-WAY 100135 (10 mg/kg) exhibited anxiolytic-like effects [2]. In free feeding rats, WAY-100135 (3 mg/kg) significantly inhibited hyperphagia and the increased incidence of feeding induced by 8-OH-DPAT (0.1 mg/kg), which was mediated by somatodendritic 5-HT1A autoreceptor [3]. In rats, (S)-WAY 100135 (0.2, 1, 5 ug/ul) inhibited the impairment of choice accuracy induced by intrahippocampal scopolamine (3.75 ug/ul) in a dose-dependent way. However, (S)-WAY 100135 didn’t influence the acquisition of spatial learning [4]. In rats, WAY-100135 (10.0 mg/kg) inhibited the decrease of 5-HT release induced by buspirone, a 5-HT1A receptor partial agonist [5].
参考文献:
[1].? Fletcher A, Bill DJ, Bill SJ, et al. WAY100135: a novel, selective antagonist at presynaptic and postsynaptic 5-HT1A receptors. Eur J Pharmacol, 1993, 237(2-3): 283-291.
[2].? Rodgers RJ, Cole JC. Anxiolytic-like effect of (S)-WAY 100135, a 5-HT1A receptor antagonist, in the murine elevated plus-maze test. Eur J Pharmacol, 1994, 261(3): 321-325.
[3].? Hartley JE, Fletcher A. The effects of WAY-100135 and 8-hydroxy-2-(di-n-propylamino)tetralin on feeding in the rat. Eur J Pharmacol, 1994, 252(3): 329-332.
[4].? Carli M, Luschi R, Samanin R. (S)-WAY 100135, a 5-HT1A receptor antagonist, prevents the impairment of spatial learning caused by intrahippocampal scopolamine. Eur J Pharmacol, 1995, 283(1-3): 133-139.
[5].? Routledge C, Gurling J, Ashworth-Preece MA, et al. Differential effects of WAY-100135 on the decrease in 5-hydroxytryptamine release induced by buspirone and NAN-190. Eur J Pharmacol, 1995, 276(3): 281-284.
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