[The histamine H(3) receptor: a target for new drugs].
[The histamine H(3) receptor: a target for new drugs].
复制标题
[组胺H(3)受体：新药的靶标]。
DOI：
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发表时间：
2003
影响因子：
1.3
通讯作者：
J. Arrang
中科院分区：
文献类型：
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作者：
J. Arrang
组胺H3受体在大鼠脑中被鉴定为抑制组胺合成和释放的突触前自身受体。在其最近的克隆之后，超过15年后，确定了该受体的亚型、种属药理学差异和高组成活性的存在。所有这些分子发现都必须考虑到以临床应用为目的的配体的优化。它们显示了拮抗剂/反向激动剂在精神分裂症和认知和注意力缺陷的对症治疗中的作用。
The histamine H3 receptor has been identified in the rat brain as a presynaptic autoreceptor inhibiting histamine synthesis and release. Following its recent cloning, more than fifteen years later, the existence of isoforms, species pharmacological differences and the high constitutive activity of the receptor were established. All these molecular findings have to be taken into account for the optimization of the ligands aiming at a clinical use. They show the interest of antagonists/inverse agonists in the symptomatic treatment of schizophrenia and cognitive and attentional deficits.