nAChRα4&β2 x nAChRα3&β4

Last update 01 Nov 2024

Basic Info

Related Targets

nAChRα4&β2nAChRα3&β4

Drugs associated with nAChRα4&β2 x nAChRα3&β4

VMY-2-109

Target

nAChRα3&β4 x nAChRα4&β2

Mechanism

nAChRα4&β2 agonists [+1]

Active Org.-

Originator Org.

Duke University

Active Indication-

Inactive Indication

Tobacco Use Disorder

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with nAChRα4&β2 x nAChRα3&β4

100 Translational Medicine associated with nAChRα4&β2 x nAChRα3&β4

0 Patents (Medical) associated with nAChRα4&β2 x nAChRα3&β4

Literatures (Medical) associated with nAChRα4&β2 x nAChRα3&β4

01 Mar 2000·NeuropharmacologyQ2 · MEDICINE

The influence of nicotinic receptor subunit composition upon agonist, α–bungarotoxin and insecticide (imidacloprid) binding affinity

Q2 · MEDICINE

Article

Author: Stuart J. Lansdell ; Neil S. Millar

A series of cell lines stably expressing recombinant nicotinic acetylcholine receptors (nAChRs) has been established by transfection of mammalian (rat) and insect (Drosophila) nicotinic subunit cDNAs. By equilibrium radioligand binding, we have examined the influence of individual subunits upon the affinity of two nicotinic agonists (epibatidine and methylcarbamylcholine), an antagonist (the snake neurotoxin, alpha-bungarotoxin) and a recently developed chloronicotinyl insecticide (imidacloprid). Imidacloprid bound with very low affinity to the rat alpha4/beta2 nAChR but did so with high affinity to hybrid nAChRs containing Drosophila alpha subunits co-assembled with rat beta2. Of the subunit combinations examined, imidacloprid showed highest affinity binding to nAChRs containing the recently identified Drosophila alpha subunit, D alpha3, co-assembled with beta2. In contrast, no specific binding of imidacloprid was detected when D alpha3 was co-expressed with the mammalian neuronal beta4 subunit, or with the muscle-type (gamma or delta) subunits. However, despite the absence of imidacloprid binding to D alpha3/beta4, D alpha3/gamma or D alpha3/delta, these subunit combinations all exhibited high affinity binding of other nicotinic radioligands. Epibatidine showed substantially higher affinity binding to subunit combinations containing neuronal (beta2 or beta4) subunits than it did to combinations containing muscle-type (gamma or delta) subunits. In contrast, alpha-bungarotoxin bound with higher affinity to combinations containing muscle-type subunits. Our results demonstrate that both alpha and non-alpha subunits exert a profound influence upon the affinity of nicotinic ligands for recombinant nAChRs.

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