U-92016A 是一种有效的、代谢稳定的、具有口服活性的 5-HT1A 受体激动剂，具有极高的内在活性。
| Cas No. | 149654-41-1 |
| 化学名 | (8R)-8-(dipropylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-2-carbonitrile, monohydrochloride |
| Canonical SMILES | CCCN(CCC)[C@@H](C1)CCC2=C1C(C=C(C#N)N3)=C3C=C2.Cl |
| 分子式 | C19H25N3.HCl |
| 分子量 | 331.9 |
| 溶解度 | DMF: 5 mg/ml,DMSO: 20 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 0.1 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | U-92016A is an agonist of the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 0.4 nM). It is selective for 5-HT1A over 5-HT1D, 5-HT2, dopamine D1 and D2, and α1- and α2-adrenergic receptors (Kis = 7.7, >1,000, >1,000, 36, >1,000, and >1,000 nM, respectively). U-92016A inhibits forskolin-stimulated cAMP synthesis in CHO cells transfected with human 5-HT1A. In vivo, U-92016A induces hypothermia in mice (ED50 = 0.041 mg/kg). It induces 5-HT syndrome, as measured by increased flat body posture and reciprocal forepaw treading, as well as decreases accumulation of 5-HT and dopamine in rats when administered at a dose of 5 mg/kg. U-92016A also decreases arterial blood pressure and heart rate in a dose-dependent manner in spontaneously hypertensive rats and reverses isolation-induced aggression in mice. |
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