The relationship of varenicline agonism of α4β2 nicotinic acetylcholine receptors and nicotine-induced dopamine release in nicotine dependent humans.

08:00 EDT 16th May 2019 | BioPortfolio

Summary of "The relationship of varenicline agonism of α4β2 nicotinic acetylcholine receptors and nicotine-induced dopamine release in nicotine dependent humans."

Cigarette smoking continues to be one of the most important behavioral causes of morbidity and mortality in the world. Varenicline, an α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist, has been shown to increase smoking quit rates compared with nicotine-based products. This human laboratory, double-blind, placebo-controlled study examined varenicline and placebo effects on α4β2-nAChRs occupancy, nicotine-induced change in [11C]raclopride binding potential (BPND) and behavioral measures of cigarette smoking, nicotine craving, and withdrawal.


Journal Details

This article was published in the following journal.

Name: Nicotine & tobacco research : official journal of the Society for Research on Nicotine and Tobacco
ISSN: 1469-994X


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Medical and Biotech [MESH] Definitions

Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.

Nicotine is highly toxic alkaloid. It is the prototypical agonist at nicotinic cholinergic receptors where it dramatically stimulates neurons and ultimately blocks synaptic transmission. Nicotine is also important medically because of its presence in tobacco smoke.

A class of insecticides that are structurally similar to NICOTINE and have physiologically similar effects as agonists of NICOTINIC ACETYLCHOLINE RECEPTORS, but are less toxic to vertebrates. They are widely used in agriculture.

One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for nicotine over muscarine. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, molecular biology, and biophysical properties of the channels.

Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.

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