螺哌丙苯

生物活性靶点体外研究体内研究螺哌丙苯试剂级价格

螺哌丙苯

CAS号:510-74-7
英文名:AMI-193
中文名:螺哌丙苯
CBNumber:CB2728009
分子式:C22H26FN3O2
分子量:383.46
MOL File:510-74-7.mol

螺哌丙苯化学性质

熔点 :176 - 179°C
储存条件 :Store at RT
溶解度 :DMSO (Slightly), Methanol (Slightly)
形态 :White solid.
颜色 :Off-White to Pale Yellow

螺哌丙苯性质、用途与生产工艺

生物活性 Spiramide (AMI-193) 是一种有效和选择性的 5-HT2 和 dopamine D2 受体拮抗剂，Ki 值分别为 2 nM 和 3 nM。Spiramide 对 5-HT2 受体的选择性与 5-HT1C 受体 (Ki=4300 nM) 相比大于 2000 倍。Spiramide 具有抗精神病活性。

靶点

5-HT ₂ Receptor

2 nM (Ki)

D ₂ Receptor

3 nM (Ki)

5-HT _1A Receptor

50 nM (Ki)

D ₁ Receptor

2530 nM (Ki)

5-HT _1C Receptor

4300 nM (Ki)

体外研究

Spiramide retains affinity for 5-HT _1A sites (K _i =50 nM) and also binds at dopamine D2 sites (K _i =3 nM), but possesses low affinity for dopamine D1 sites (K _i =2530 nM).

体内研究

AMI-193 (0.003-0.01 mg/kg; i.m.) dose-dependently decreases response rate in monkeys under a fixed-interval (FI) schedule of stimulus termination.
AMI-193 (0.003-0.01 mg/kg; i.m.) attenuates the discriminative-stimulus effects of cocaine in drug-discrimination experiments.
AMI-193 (0.003-0.01 mg/kg; i.m.) reduces response rate under a second-order schedule of i.v. self-administration of cocaine (0.1 mg/infusion).

Animal Model:	Adult male squirrel monkeys (850-1300 g)
Dosage:	0.003, 0.01 mg/kg
Administration:	I.m. on Tuesday, Wednesday, and Thursday the following week
Result:	Decreased the response rate. The rate-decreasing effects were reversed by cocaine.