Neuroleptic binding to muscarinic M2 receptors of normal human heart in vitro and comparison with binding to M1 and dopamine D2 receptors of brain.

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Neeper R, Richelson E, Nelson A

Neuroleptic binding to muscarinic M2 receptors of normal human heart in vitro and comparison with binding to M1 and dopamine D2 receptors of brain.

Neuropharmacology. 1991 May;30(5):527-9.

PubMed ID

1678146 [ View in PubMed

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Abstract

We determined by radioligand binding the equilibrium dissociation constants (Kd's) for seventeen neuroleptics at muscarinic M2 receptors of human heart atrium and compared these data with our previous data for binding to muscarinic M1 and dopamine D2 receptors of human brain. At the M2 receptor, the most potent compound was thioridazine; the least, molindone. If selectivity is defined as Kd at one receptor less than or equal to 0.1 Kd at the other receptor, no compound was selective for the M2 subtype. Two compounds, clozapine and triflupromazine, were selective for the M1 subtype. Thus, few neuroleptics have the assumed preferred property of M1 over M2 subtype selectivity. Such a feature could reduce extrapyramidal side effects, while reducing the likelihood of certain cardiac side effects.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Molindone	Muscarinic acetylcholine receptor M1	Protein	Humans	Unknown	Other/unknown	Details