Beta-subunits co-determine the sensitivity of rat neuronal nicotinic receptors to antagonists.

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Cachelin AB, Rust G

Beta-subunits co-determine the sensitivity of rat neuronal nicotinic receptors to antagonists.

Pflugers Arch. 1995 Jan;429(3):449-51.

PubMed ID

7761270 [ View in PubMed

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Abstract

We have investigated the effect of 4 ganglionic cholinergic antagonists (hexamethonium, mecamylamine, pentolinium, trimetaphan) on rat alpha 3 beta 2 and alpha 3 beta 4 neuronal nicotinic acetylcholine receptors (nAChRs) expressed in Xenopus oocytes. Current responses were elicited by fast application of acetylcholine on voltage-clamped oocytes (holding potentialVh = -80mV). Concentration-inhibition curves were used to get estimates of IC50, the antagonist concentration yielding 50% reduction of the peak current. The KB's of the antagonists were calculated using estimates of the apparent KD of acetylcholine. The order of affinity of the antagonists was similar for both receptor subtypes: mecamylamine approximately pentolinium > hexamethonium > trimetaphan. However, alpha 3 beta 4 neuronal nAChRs were 9 to 22 times more sensitive to each of the 4 antagonists than alpha 3 beta 2 receptors. These results further underline the importance of the beta-subunit as co-determinant of the functional properties of neuronal nAChRs.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Pentolinium	Neuronal acetylcholine receptor subunit alpha-10	Protein	Humans	Yes	Antagonist	Details
Pentolinium	Neuronal acetylcholine receptor subunit alpha-3	Protein	Humans	Yes	Antagonist	Details
Pentolinium	Neuronal acetylcholine receptor subunit beta-4	Protein	Humans	Yes	Antagonist	Details