5-HT1A modulator 1 对 5HT_1A，肾上腺素能 α₁ 和多巴胺 D₂ 受体具有非常高的亲和力，IC₅₀ 分别为 2±0.3 nM，10±3 nM 和 40±9 nM。

5-HT1A modulator 1 displays very high affinities for the 5HT 1A , adrenergic α 1 and dopamine D 2 receptor with IC 50 s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.

Solid

sPLA2 2 nM (IC50) 5-HT2A Receptor

5-HT1A modulator 1 (Compound 24) also displays affinities for the 5HT1B, 5-HT2A and 5-HT2C receptor with IC50s of 300±55 nM, 500±75 nM, and 4000±440 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.

5-HT1A modulator 1 (Compound 24) shows clear antagonist action at 5HT 2A receptor subtype in mice. The antagonism is nearly complete at the dose of 1 mg/kg ip for 5-HT1A modulator 1 (94% of antagonism, p<0.01). 5-HT1A modulator 1 completely blocks the stereotypies and the climbing at the dose of 1 mg/kg ip (100% of antagonism). 5-HT1A modulator 1 is also tested in rats, using the same paradigm. After oral administration, 5-HT1A modulator 1 significantly (p<0.05) reduces the hyperactivity by 50% at the doses of 2 and 4 mg/kg po, respectively 63% and 58% of antagonism for 5-HT1A modulator 1; the antagonism is complete (103% and 108%) at the respective doses of 8 and 16 mg/kg po for 5-HT1A modulator 1 (p<0.01). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Taverne T, et al. Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. J Med Chem. 1998 Jun 4;41(12):2010-8.