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首页> 外文期刊>CNS drug reviews >Pharmacology of the beta-carboline FG-7,142, a partial inverse agonist at the benzodiazepine allosteric site of the GABA A receptor: neurochemical, neurophysiological, and behavioral effects.
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Pharmacology of the beta-carboline FG-7,142, a partial inverse agonist at the benzodiazepine allosteric site of the GABA A receptor: neurochemical, neurophysiological, and behavioral effects.

机译：β-咔啉FG-7,142（在GABA A受体的苯二氮卓别构部位的部分反向激动剂）的药理作用：神经化学，神经生理学和行为学作用。

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Given the well-established role of benzodiazepines in treating anxiety disorders, beta-carbolines, spanning a spectrum from full agonists to full inverse agonists at the benzodiazepine allosteric site for the GABA(A) receptor, can provide valuable insight into the neural mechanisms underlying anxiety-related physiology and behavior. FG-7,142 is a partial inverse agonist at the benzodiazepine allosteric site with its highest affinity for the alpha1 subunit-containing GABA(A) receptor, although it is not selective. FG-7,142 also has its highest efficacy for modulation of GABA-induced chloride flux mediated at the alpha1 subunit-containing GABA(A) receptor. FG-7,142 activates a recognized anxiety-related neural network and interacts with serotonergic, dopaminergic, cholinergic, and noradrenergic modulatory systems within that network. FG-7,142 has been shown to induce anxiety-related behavioral and physiological responses in a variety of experimental paradigms across numerous mammalian and non-mammalian species, including humans. FG-7,142 has proconflict actions across anxiety-related behavioral paradigms, modulates attentional processes, and increases cardioacceleratory sympathetic reactivity and neuroendocrine reactivity. Both acute and chronic FG-7,142 treatment are proconvulsive, upregulate cortical adrenoreceptors, decrease subsequent actions of GABA and beta-carboline agonists, and increase the effectiveness of subsequent GABA(A) receptor antagonists and beta-carboline inverse agonists. FG-7,142, as a partial inverse agonist, can help to elucidate individual components of full agonism of benzodiazepine binding sites and may serve to identify the specific GABA(A) receptor subtypes involved in specific behavioral and physiological responses.
机译：鉴于苯二氮卓类药物在治疗焦虑症中已确立的作用，β-咔啉在GABA（A）受体的苯二氮卓类变构位点上涵盖从完全激动剂到完全反向激动剂的整个范围，可以为了解焦虑背后的神经机制提供有价值的见解相关的生理和行为。 FG-7,142是苯并二氮杂构变构位点的部分反向激动剂，对含α1亚基的GABA（A）受体具有最高亲和力，尽管它不是选择性的。 FG-7,142在调节GABA诱导的含α1亚基的GABA（A）受体介导的氯离子通量方面也具有最高功效。 FG-7,142激活公认的与焦虑相关的神经网络，并与该网络内的血清素能，多巴胺能，胆碱能和去甲肾上腺素能调节系统相互作用。 FG-7,142已被证明可以在包括人类在内的众多哺乳动物和非哺乳动物物种的各种实验范例中诱发与焦虑相关的行为和生理反应。 FG-7,142具有与焦虑相关的行为范式的冲突行为，调节注意力过程，并增加了心脏加速交感反应性和神经内分泌反应性。急性和慢性FG-7,142治疗都是惊厥性的，上调皮质肾上腺素受体，减少GABA和β-咔啉激动剂的后续作用，并提高随后的GABA（A）受体拮抗剂和β-咔啉反向激动剂的有效性。 FG-7,142作为部分反向激动剂，可以帮助阐明苯二氮卓结合位点完全激动的各个成分，并可能有助于鉴定参与特定行为和生理反应的特定GABA（A）受体亚型。

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