AMI-193
(Synonyms: 螺哌丙苯,AMI-193) 目录号 : GC16049
AMI-193 (AMI-193) 是一种有效的、选择性的 5-HT2 和多巴胺 D2 受体拮抗剂,Kis 分别为 2 nM 和 3 nM。
Cas No.:510-74-7
Sample solution is provided at 25 µL, 10mM.
AMI-193 is a potent and selective antagonist of 5-HT2A receptor and dopamine D2-receptor with Ki values of 2 and 3 nM, respectively [1].
The 5-HT2A receptor is a G protein-coupled receptor and a subtype of the 5-HT2 receptor. The 5-HT2A receptor plays an important role in the spread of the human polyoma virus. The dopamine D2-receptor is a G protein-coupled receptor that inhibits adenylyl cyclase activity.
AMI-193 is a potent and selective 5-HT2A receptor and dopamine D2-receptor antagonist. AMI-193 was highly selective for 5-HT2A versus 5-HT2C receptor with Ki values of 2 and 4300 nM for 5-HT2A and 5-HT2C receptor, respectively [1]. Also, AMI-193 bound to 5-HT2 receptor with Ki value of 2 nM and exhibited >2000-fold selectivity versus 5-HT1C receptor. In cortical slices, AMI-193 (10-10 - 10-5 M) inhibited GABA release in a dose-dependent way and increased 5-HT outflow [3].
In rats, AMI-193 behaved as an antagonist with ED50 value of 0.003 mg/kg [2].
References:
[1]. Czoty PW, Howell LL. Behavioral effects of AMI-193, a 5-HT(2A)- and dopamine D(2)-receptor antagonist, in the squirrel monkey. Pharmacol Biochem Behav, 2000, 67(2): 257-264.
[2]. Ismaiel AM, De Los Angeles J, Teitler M, et al. Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist. J Med Chem, 1993, 36(17): 2519-2525.
[3]. Luparini MR, Garrone B, Pazzagli M, et al. A cortical GABA-5HT interaction in the mechanism of action of the antidepressant trazodone. Prog Neuropsychopharmacol Biol Psychiatry, 2004, 28(7): 1117-1127.
Cas No. | 510-74-7 | SDF | |
别名 | 螺哌丙苯,AMI-193 | ||
化学名 | 8-(3-(4-fluorophenoxy)propyl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one | ||
Canonical SMILES | FC1=CC=C(C=C1)OCCCN2CC[C@]3(CC2)N(C4=CC=CC=C4)CNC3=O | ||
分子式 | C22H26FN3O2 | 分子量 | 383.46 |
溶解度 | <28.76mg/ml in DMSO | 储存条件 | Store at RT |
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1 mg | 5 mg | 10 mg |
1 mM | 2.6078 mL | 13.0392 mL | 26.0783 mL |
5 mM | 0.5216 mL | 2.6078 mL | 5.2157 mL |
10 mM | 0.2608 mL | 1.3039 mL | 2.6078 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.50%
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