耗材描述
Spiramide
产品活性: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。
产品来源: https://www.medchemexpress.cn/spiramide.html
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:5-HT Receptor | Dopamine Receptor
来源:植物 | 蔷薇科 | 粉花绣线菊
结构分类:生物碱 | 哌啶类生物碱
In Vitro: Spiramide retains affinity for 5-HT1A sites (Ki=50 nM) and also binds at dopamine D2 sites (Ki=3 nM), but possesses low affinity for dopamine D1 sites (Ki=2530 nM).
In Vivo: 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).
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