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Muscarinic acetylcholine receptors possess a regulatory effect on dopaminergic neurotransmission. Activation of M 4 receptors in the striatum inhibit D 1-induced locomotor stimulation in mice. M 4 receptor-deficient mice exhibit increased locomotor simulation in response to D 1 agonists, amphetamine and cocaine.
Muscarinic acetylcholine receptors (mAChRs) are acetylcholine receptors that form G protein-coupled receptor complexes in the cell membranes of certain neurons [1] and other cells. They play several roles, including acting as the main end-receptor stimulated by acetylcholine released from postganglionic fibers .
A muscarinic acetylcholine receptor agonist, also simply known as a muscarinic agonist or as a muscarinic agent, is an agent that activates the activity of the muscarinic acetylcholine receptor. [1] The muscarinic receptor has different subtypes, labelled M1-M5, allowing for further differentiation.
PD-102,807 is a drug which acts as a selective antagonist for the muscarinic acetylcholine receptor M 4. [1] [2] [3] It is used in scientific research for studying the effects of the different muscarinic receptor subtypes in the body and brain. [4] [5] [6] [7]
PD-0298029 is a drug which acts as a selective antagonist for the muscarinic acetylcholine receptor M 4. It was developed for the treatment of Parkinson's disease, but poor bioavailability and rapid metabolism in animal studies have meant its use is largely limited to in vitro research into the M 4 and other muscarinic receptors. [1] [2] [3]
NS-136 is a selective muscarinic acetylcholine M 4 receptor positive allosteric modulator which is under development for the treatment of schizophrenia and Alzheimer's disease. [1] [3] [2] It has been found to possess pro-cognitive effects in rodents. [2] The drug is under development by NeuShen Therapeutics.
This page was last edited on 24 September 2018, at 18:00 (UTC).; Text is available under the Creative Commons Attribution-ShareAlike 4.0 License; additional terms may apply.
[1] [2] As of August 2024, it is in phase 2 clinical trials. [1] [3] Emraclidine is a positive allosteric modulator that selectively targets the muscarinic acetylcholine receptor M4 subtype. The M4 receptor subtype is expressed in the striatum of the brain, which plays a key role in regulating acetylcholine and dopamine levels. An imbalance of ...