Langer Salomon Z
Alpha-2 Pharmaceutica AB, 8 Rosemblum Street, Apt. 4650, Tel Aviv 69379, Israel.
Neurochem Int. 2008 Jan;52(1-2):26-30. doi: 10.1016/j.neuint.2007.04.031. Epub 2007 May 16.
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.
35年前发现突触前神经末梢的细胞质膜拥有调节神经递质释放的受体。这一新概念明显背离了传统观点，即神经元通信是单向的，也就是从神经末梢到突触后受体，因为通过突触前受体进行的信息传递方向相反：从突触间隙到释放神经递质的神经末梢。突触前释放调节自身受体和异源受体是外源性化合物作为激动剂、部分激动剂或拮抗剂进行药理干预的合适靶点。这类化合物可能具有治疗价值，因为它们可通过突触前影响递质释放，且比使用激动剂或拮抗剂药物刺激或阻断突触后受体这种成熟方法产生的副作用更少。
