Human presynaptic receptors

doi:10.1016/j.pharmthera.2016.11.005

2017-04-01

PRE

Eberhard Schlicker *

Thomas J. Feuerstein

DOI：10.1016/j.pharmthera.2016.11.005

原文链接

原文求助

摘要

En 中文

Presynaptic receptors are sites at which transmitters, locally formed mediators or hormones inhibit or facilitate the release of a given transmitter from its axon terminals. The interest in the identification of presynaptic receptors has faded in recent years and it may therefore be justified to give an overview of their occurrence in the autonomic and central nervous system; this review will focus on presynaptic receptors in human tissues. Autoreceptors are presynaptic receptors at which a given transmitter restrains its further release, though in some instances may also increase its release. Inhibitory autoreceptors represent a typical example of a negative feedback; they are tonically activated by the respective endogenous transmitter and/or are constitutively active. Autoreceptors also play a role under pathophysiological conditions, e.g. by limiting the massive noradrenaline release occurring during congestive heart failure. They can be used for therapeutic purposes; e.g., the alpha(2)-adrenoceptor antagonist mirtazapine is used as an antidepressant and the inverse histamine H-3 receptor agonist pitolisant has been marketed as a new drug for the treatment of narcolepsy in 2016. Heteroreceptors are presynaptic receptors at which transmitters from adjacent neurons, locally formed mediators (e.g. endocannabinoids) or hormones (e.g. adrenaline) can inhibit or facilitate transmitter release; they may be subject to an endogenous tone. The constipating effect of the sympathetic nervous system or of the anti hypertensive drug clonidine is related to the activation of inhibitory alpha(2)-adrenoceptors on postganglionic parasympathetic neurons. Part of the stimulating effect of adrenaline on the sympathetic nervous system during stress is related to its facilitatory effect on noradrenaline release via alpha(2)-adrenoceptors. (C) 2016 Elsevier Inc. All rights reserved.

Keyword:

Monoaminergic neurons

Cholinergic neurons

GABAergic neurons

Glutamatergic neurons

Modulation of transmitter release

Induction of transmitter release