阿片受体的双重性、变构调节和偏向性信号传导:未来的治疗潜力。

A.M. González, A.G. Jubete
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引用次数: 0

摘要

阿片类药物仍然是治疗急性术后疼痛和慢性癌症疼痛的首选药物。这些药物的过量用药在一些国家引发了“阿片类药物危机”。在这种情况下,人们已经注意到各种配体的治疗潜力,这些配体充当正构结合位点的变构调节剂,并调节药物的活性、亲和力、效力甚至疗效。
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Dualism, allosteric modulation, and biased signaling of opioid receptors: Future therapeutic potential

Opioids are still the drugs of choice for the treatment of acute post-surgical pain and chronic cancer pain. Overprescribing of these drugs has given rise to an “opioid crisis” in some countries. In this context, attention has been drawn to the therapeutic potential of various ligands that act as allosteric modulators of orthosteric binding sites and modulate the drug’s activity, affinity, potency, and even efficacy.

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