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510-74-7

中文名稱 螺哌丙苯
英文名稱 AMI-193
CAS 510-74-7
分子式 C22H26FN3O2
分子量 383.46
MOL 文件 510-74-7.mol
更新日期 2023/03/20 15:41:27
510-74-7 結(jié)構(gòu)式 510-74-7 結(jié)構(gòu)式

基本信息

中文別名
螺哌丙苯
螺拉米特
英文別名
R 5808
AMI-193
spiramide
Fluroxyspiramine
8-[3-(4-FLUOROPHENOXY)PROPYL]-1-PHENYL-1,3,8-TRIAZASPIRO[4.5]-DECANONE
8-[3-(4-FLUOROPHENOXY)PROPYL]-1-PHENYL-1,3,8-TRIAZASPIRO[4.5]DECAN-4-ONE
1-Phenyl-8-[3-(4-fluorophenoxy)propyl]-1,3,8-triazaspiro[4.5]decane-4-one
1,3,8-Triazaspiro[4.5]decan-4-one, 8-[3-(4-fluorophenoxy)propyl]-1-phenyl-

物理化學性質(zhì)

熔點176 - 179°C
儲存條件Store at RT
溶解度可溶于DMSO(少許)、甲醇(少許)
形態(tài)白色固體。
顏色灰白色至淡黃色
螺哌丙苯價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-100971螺哌丙苯
Spiramide
510-74-75mg800元
2024/11/08HY-100971螺哌丙苯
Spiramide
510-74-710mM * 1mLin DMSO880元
2024/11/08HY-100971螺哌丙苯
Spiramide
510-74-710mg1300元

常見問題列表

生物活性
Spiramide (AMI-193) 是一種有效和選擇性的 5-HT2 和 dopamine D2 受體拮抗劑,Ki 值分別為 2 nM 和 3 nM。Spiramide 對 5-HT2 受體的選擇性與 5-HT1C 受體 (Ki=4300 nM) 相比大于 2000 倍。Spiramide 具有抗精神病活性。
靶點

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)

體外研究

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).

體內(nèi)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.
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