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5-HT(7) Receptors.

机译：5-HT（7）受体。

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Following the cloning of the 5-HT(7) receptor in 1993, studies to investigate 5-HT(7) receptor function in native tissues focused on identifying functional correlates that matched the pharmacological profile determined for the cloned receptor. Studies in peripheral tissues established that the 5-HT(7) receptor mediates the relaxation of smooth muscle, including the gastrointestinal tract and cardiovascular systems. Although a number of studies provided preliminary evidence for a role for the 5-HT(7) receptor in the circadian pacemaker function of the suprachiasmatic nucleus (SCN), additional studies to investigate 5-HT(7) receptor function in other brain regions have, until recently, been hindered by the absence of 5-HT(7) receptor-selective ligands. More recently, a number of 5-HT(7) receptor-selective antagonists including, SB-269970-A and SB-656104-A have been developed. Studies utilising these compounds suggest that the 5-HT(7) receptor modulates neuronal function in a number of brain areas including the hippocampus and thalamus. In turn, these findings suggest that 5-HT(7) receptor-selective ligands might prove therapeutically useful for the treatment of psychiatric disorders. In this respect there is increasing evidence to suggest that the 5-HT(7) receptor plays a role in the control of both circadian rhythms and sleep and might therefore represent a therapeutic target for the treatment of those disorders in which disturbances in circadian rhythms and sleep architecture are thought to be contributory factors. Furthermore, there is evidence to suggest that the receptor may play a role in other CNS disorders including, anxiety, cognitive disturbances and also migraine probably via both peripheral and central mechanisms. Although further studies are required to confirm the potential role of the receptor in such disorders, findings to date suggest there are exciting opportunities for the development of novel therapeutic agents acting either selectively at the 5-HT(7) receptor or whose profile of action includes an interaction with this receptor.
机译：在1993年克隆了5-HT（7）受体后，研究了在天然组织中研究5-HT（7）受体功能的研究重点是确定与为克隆的受体确定的药理特性相匹配的功能相关性。在外围组织中的研究表明，5-HT（7）受体可介导平滑肌的松弛，包括胃肠道和心血管系统。尽管许多研究为5-HT（7）受体在视交叉上核（SCN）的昼夜节律起搏器功能中的作用提供了初步的证据，但其他研究5-HT（7）受体在其他脑区的功能的研究直到最近，由于没有5-HT（7）受体选择性配体而受到阻碍。最近，已开发出许多5-HT（7）受体选择性拮抗剂，包括SB-269970-A和SB-656104-A。利用这些化合物的研究表明，5-HT（7）受体可调节包括海马和丘脑在内的许多大脑区域的神经元功能。反过来，这些发现表明5-HT（7）受体选择性配体可能被证明在治疗精神疾病方面具有治疗作用。在这方面，越来越多的证据表明5-HT（7）受体在控制昼夜节律和睡眠中均起着作用，因此可能代表治疗那些昼夜节律和睡眠障碍的疾病的治疗靶标。睡眠结构被认为是促成因素。此外，有证据表明该受体可能在其他中枢神经系统疾病中起作用，包括焦虑，认知障碍以及偏头痛，可能是通过外围和中枢机制。尽管需要进一步的研究来确认受体在此类疾病中的潜在作用，但迄今为止的发现表明，开发选择性作用于5-HT（7）受体或作用机理包括与该受体的相互作用。

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