5-HT1A modulator 1 对 5HT1A，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。
| 生物活性 |
5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively. |
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| IC50&Target |
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| 体外研究 |
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. |
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| 体内研究 |
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).
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| 分子量 |
383.51
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| CAS号 |
142477-34-7
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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纯度： 97%
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