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A study of bile acids as opioid receptor ligands in rat brain membranes.

机译:胆汁酸作为大鼠脑膜中阿片样物质受体配体的研究。

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摘要

There is evidence to suggest that the pruritus that results from liver disease is mediated, at least in part, by opioid receptor-ligand interactions; a central component has been proposed. Opiate drugs with agonist activity at opioid receptors induce naloxone-reversible pruritus. Bile acids accumulate in tissues in liver disease. We studied the ability of bile acids to displace specific opioid ligands from opioid receptors in rat and guinea pig brain membrane preparation in binding assays. None of the bile acids studied displaced significantly the opioid ligands from their receptors suggesting that bile acids in vitro are not opioid receptor ligands. The results of this study do not support a role of these bile acids as direct pruritogens by an opioid receptor-mediated mechanism.
机译:有证据表明,由肝病引起的瘙痒至少部分是由阿片受体-配体相互作用所介导的。已经提出了一个中心组成部分。对阿片受体具有激动剂活性的阿片类药物可诱发纳洛酮可逆性瘙痒症。胆汁酸在肝脏疾病的组织中积累。在结合试验中,我们研究了胆汁酸从大鼠和豚鼠脑膜制剂中的阿片受体中置换特定阿片配体的能力。所研究的胆汁酸均未从其受体上显着替代阿片样物质配体,表明体外胆汁酸不是阿片样物质受体配体。这项研究的结果不支持通过阿片样物质受体介导的机制将这些胆汁酸作为直接的甜菜素的作用。

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