5-HT1A modulator 1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

5-HT1A 调节剂 1 对 5-HT1A、α1-肾上腺素能受体和 D2 受体表现出非常高的亲和力。

5-HT1A modulator 1 displays very high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).(In Vitro):5-HT1A modulator 1 displays affinities for the 5-HT1B, 5-HT2A, and 5-HT2C (IC50s = 300 nM, 500 nM, and 4000 nM).(In Vivo):5-HT1A modulator 1 (1 mg/kg; i.p) shows 94% antagonist action at 5-HT2A subtype in mice. 5-HT1A modulator 1 (1 mg/kg; i.p) completely blocks the stereotypes and the climbing. In rats, 5-HT1A modulator 1 (2 and 4 mg/kg; p.o) shows a respective 63% and 58% of antagonism and the antagonism is complete (103% and 108%) at doses of 8 and 16 mg/kg. 5-HT1A modulator 1 significantly reduces hyperactivity by 50%.

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.

5-HT1A modulator 1 (Compound 24) shows clear antagonist action at 5HT2A 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).

5-HT1Amodulator1

Metabolic Enzyme/Protease

Phospholipase

PROTAC Linker

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142477-34-7

383.51

C21H25N3O2S

>98% (HPLC)

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COc1ccccc1N1CCN(CCc2ccc3n(C)c(=O)sc3c2)CC1

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(-20℃)

With Ice Pack

≥ 2 years