熔点 | 196-198 °C |
溶解性 | Soluble in DMSO (~10 mg/ml), ethanol (~10 mg/ml), DMF (~10 mg/ml), and 1:3 DMSO:PBS (pH 7.2) (~14 mg/ml). Insoluble in water |
存贮条件 | 储存温度 2-8°C |
应用 | An inverse agonist of the CB1 receptor;AM251, a CB1 cannabinoid receptor antagonist, has been used in a study to determine its interaction with hippocampal neurons to enhance spatial memory in mice. |
产品介绍 | AM251是大麻素CB1受体拮抗剂,IC50为700 nM,在体内与小鼠脑CB1受体结合。 |
备注 | AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain. |
生化机理 | AM-251 is a 123I radioisotope and potent CB1 receptor antagonist derivative of the CB1 cannabinoid receptor inverse agonist SR141716A, presenting a radioprobe for in vivo binding studies at the CB1 receptor with a higher affinity (Ki = 7.49 nM) for CB1 than the parent compound (Ki = 11.5 nM). AM-251 has been employed in competitive binding studies to identify CB1 affinity of different cannabimimetic agonists in vivo. Characterization of AM-251-CB1 association with SPECT (single photon emission computed tomography) has been described. AM-251 is also a potent activator of the GPR55 receptor. |
别名 | 1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-1-哌啶基-1H-吡唑-3-甲酰胺;AM 251;AM-251;1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-carboxamide;AM 251;AM-251 |
AM251,CB 1受体拮抗剂/反向激动剂
AM251 (订货以英文为准)
编号:A129844
CAS号:183232-66-8
分子式:C22H21CL2IN4O
分子量:555.24
产品名称 | AM251 |
中文名称 | AM251,CB 1受体拮抗剂/反向激动剂 |
CAS号 | 183232-66-8 |
分子式(M.F.) | C22H21CL2IN4O |
分子量(M.W.) | 555.24 |
储存条件 | 2-8°C储存 |
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