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Presynaptic autoreceptors regulating transmitter release.

机译:突触前自动受体调节递质的释放。

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摘要

The discovery that the cytoplasmic membrane of presynaptic nerve terminals possess receptors that modulates release of neurotransmitters was made 35 years ago. This new concept represents a clear departure from the traditional view that neuronal communication was unidirectional, i.e. from the nerve terminal to the postsynaptic receptor, because the transfer of information via presynaptic receptors occurs in the opposite direction: from the synaptic cleft to the nerve terminals which release the neurotransmitter. Presynaptic release-modulating autoreceptors and heteroreceptors represent suitable targets for pharmacological intervention by exogenous compounds acting as agonists, partial agonists or antagonists. Such compounds may be of therapeutic value by influencing transmitter release presynaptically, and having fewer side effects than the well-established approach of using agonists or antagonist drugs to stimulate or block postsynaptic receptors.
机译:突触前神经末梢的细胞质膜具有调节神经递质释放的受体是35年前的发现。这个新概念与传统观点(即神经元交流是单向的,即从神经末梢到突触后受体)的观点明显不同,因为通过突触前受体的信息传递方向相反:从突触裂隙到神经末梢释放神经递质。突触前释放调节自体受体和异体受体代表通过用作激动剂,部分激动剂或拮抗剂的外源化合物进行药理干预的合适靶标。此类化合物可通过突触地影响递质释放而具有治疗价值,并且与使用激动剂或拮抗剂药物刺激或阻断突触后受体的公认方法相比,副作用较小。

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