| 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 |
