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CGP7930: a positive allosteric modulator of the GABAB receptor.

机译：CGP7930：GABAB受体的正变构调节剂。

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摘要

CGP7930 (3-(3',5'-Di-tert-butyl-4'-hydroxy)phenyl-2,2-dimethylpropanol) is a positive allosteric modulator of the metabotropic GABAB receptor. CGP7930 has been found to modulate the GABAB receptor in the open, or high affinity, state increasing agonist affinity for the receptor and signal transduction efficacy following agonist stimulation. The GABAB heteromeric subunit B2, involved in signal transduction but not ligand binding, seems to be the site of action of CGP7930 and similar allosteric modulators. When administered alone in naive animals, CGP7930 acts as an anxiolytic in rodents without other overt behavioral effects and has also been demonstrated to reduce self-administration of nicotine, cocaine, or alcohol in rodents, suggesting that "fine tuning" of the GABAB receptor by positive allosteric modulators may be able to regulate abuse of these drugs. Baclofen, the GABAB agonist, is currently finding use in treating addiction and various other disorders, but this can result in off-target effects and tolerance. CGP7930 when co-administered with baclofen enhances its potency, which could in theory minimize deleterious effects. Further study of CGP7930 is required, but this compound, and others like it, holds potential in a clinical setting.
机译：CGP7930（3-（3'，5'-二叔丁基-4'-羟基）苯基-2,2-二甲基丙醇）是代谢型GABA B受体的正变构调节剂。已经发现CGP7930以开放的或高亲和力的状态调节GABA B受体，对受体的激动剂亲和力增加，并且在激动剂刺激后信号转导效力。参与信号转导但不参与配体结合的GABA B异聚亚基B2似乎是CGP7930和类似变构调节剂的作用位点。当在幼稚动物中单独施用时，CGP7930可以在啮齿动物中发挥抗焦虑作用，而没有其他明显的行为影响，并且还被证明可以减少啮齿动物中尼古丁，可卡因或酒精的自我施用，这表明GABAB受体可以“微调”积极的变构调节剂可能能够调节这些药物的滥用。 GABAB激动剂巴氯芬目前正在用于治疗成瘾和各种其他疾病，但这可能导致脱靶效应和耐受性。 CGP7930与巴氯芬合用时，可增强其效价，从理论上讲，可将有害作用降至最低。需要对CGP7930进行进一步的研究，但该化合物及其他类似化合物在临床上具有潜力。

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