Endothelium-dependent relaxation in response to acetylcholine in the human uterine artery.

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Jovanovic A, Grbovic L, Tulic I

Endothelium-dependent relaxation in response to acetylcholine in the human uterine artery.

Eur J Pharmacol. 1994 Apr 21;256(2):131-9.

PubMed ID

8050463 [ View in PubMed

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Abstract

The effect of acetylcholine on isolated human uterine artery rings was investigated. Acetylcholine induced concentration and endothelium-dependent relaxation (pD2 = 7.29 +/- 0.03) of the precontracted arterial segments. The dissociation constant (KA) for acetylcholine was 1.35 (0.92-1.77) mumol/l. The occupancy-response relationship was non-linear. Half-maximal response to acetylcholine was obtained with 5.25% receptor occupancy. Muscarinic receptor antagonists: atropine, pirenzepine, methoctramine, p-fluoro-hexahydro-sila-diphenidol (pFHHSiD) and 4-diphenyl-acetoxy-N-methyl-piperidine (4-DAMP) competitively antagonized the response to acetylcholine. The constrained pA2 values were 9.32 +/- 0.03, 7.13 +/- 0.01, 6.26 +/- 0.01, 8.17 +/- 0.01 and 9.13 +/- 0.02, respectively. A selective muscarinic M2 receptor antagonist, gallamine, had no effect on acetylcholine-induced relaxation. It is concluded that in human uterine arteries acetylcholine induces endothelium-dependent relaxation and acts as a full agonist. We suggest that the muscarinic receptors involved in the acetylcholine-induced relaxation of the isolated human uterine artery are predominantly of the M3 subtype.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Diphenidol	Muscarinic acetylcholine receptor M2	Protein	Humans	Yes	Antagonist	Details