Abstract
The role of muscarinic and nicotinic cholinergic receptors in analgesia and neuropathic pain relief is relatively unknown. This review describes how such drugs induce analgesia or alleviate neuropathic pain by acting on the central cholinergic system. Several pharmacological strategies are discussed which increase synthesis and release of acetylcholine (ACh) from cholinergic neurons. The effects of their acute and chronic administration are described. The pharmacological strategies which facilitate the physiological functions of the cholinergic system without altering the normal modulation of cholinergic signals are highlighted. It is proposed that full agonists of muscarinic or nicotinic receptors should be avoided. Their activation is too intense and un-physiological because neuronal signals are distorted when these receptors are constantly activated. Good results can be achieved by using agents that are able to a) increase ACh synthesis, b) partially inhibit cholinesterase activity c) selectively block the autoreceptor or heteroreceptor feedback mechanisms.
Activation of M1 subtype muscarinic receptors induces analgesia. Chronic stimulation of nicotinic (N1) receptors has neuronal protective effects. Recent experimental results indicate a relationship between repeated cholinergic stimulation and neurotrophic activation of the glial derived neurotrophic factor (GDNF) family. At least 9 patents covering novel chemicals for cholinergic system modulation and pain control are discussed.
Keywords: Artemin (ARTN), analgesia, cholinergic drugs, cholinergic system, glial-derived neurotrophic factor, muscarinic receptors, neuropathic pain, nicotinic receptors, Analgesic and Antineuropathic Drugs, Central Cholinergic Mechanisms
Recent Patents on CNS Drug Discovery (Discontinued)
Title: Analgesic and Antineuropathic Drugs Acting Through Central Cholinergic Mechanisms
Volume: 6 Issue: 2
Author(s): Alessandro Bartolini, Lorenzo Di Cesare Mannelli and Carla Ghelardini
Affiliation:
Keywords: Artemin (ARTN), analgesia, cholinergic drugs, cholinergic system, glial-derived neurotrophic factor, muscarinic receptors, neuropathic pain, nicotinic receptors, Analgesic and Antineuropathic Drugs, Central Cholinergic Mechanisms
Abstract: The role of muscarinic and nicotinic cholinergic receptors in analgesia and neuropathic pain relief is relatively unknown. This review describes how such drugs induce analgesia or alleviate neuropathic pain by acting on the central cholinergic system. Several pharmacological strategies are discussed which increase synthesis and release of acetylcholine (ACh) from cholinergic neurons. The effects of their acute and chronic administration are described. The pharmacological strategies which facilitate the physiological functions of the cholinergic system without altering the normal modulation of cholinergic signals are highlighted. It is proposed that full agonists of muscarinic or nicotinic receptors should be avoided. Their activation is too intense and un-physiological because neuronal signals are distorted when these receptors are constantly activated. Good results can be achieved by using agents that are able to a) increase ACh synthesis, b) partially inhibit cholinesterase activity c) selectively block the autoreceptor or heteroreceptor feedback mechanisms.
Activation of M1 subtype muscarinic receptors induces analgesia. Chronic stimulation of nicotinic (N1) receptors has neuronal protective effects. Recent experimental results indicate a relationship between repeated cholinergic stimulation and neurotrophic activation of the glial derived neurotrophic factor (GDNF) family. At least 9 patents covering novel chemicals for cholinergic system modulation and pain control are discussed.
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Cite this article as:
Bartolini Alessandro, Di Cesare Mannelli Lorenzo and Ghelardini Carla, Analgesic and Antineuropathic Drugs Acting Through Central Cholinergic Mechanisms, Recent Patents on CNS Drug Discovery (Discontinued) 2011; 6 (2) . https://dx.doi.org/10.2174/157488911795933901
DOI https://dx.doi.org/10.2174/157488911795933901 |
Print ISSN 1574-8898 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3954 |
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