Characterization of the muscarinic receptors in the mesenteric vascular bed of spontaneously hypertensive rats

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Abstract

Objective:

The nature of the muscarinic (M) receptor subtype mediating endothelium-dependent vasodilation was investigated in Wistar-Kyoto (WKY) rats and spontaneously hypertensive rats (SHR)

Design:

Characterization of the muscarinic receptor mediating vasodilation and the possible hypertension-induced effects on the nature of this receptor, which have both received little attention in resistance vessels of the SHR

Methods:

After a methoxamine-induced vasoconstriction, the vessels were dilated with acetyl-β-metacholine (MCh). The MCh-induced vasodilation was analysed by means of the M1-selective antagonist pirenzepine, the M2-selective antagonists AF-DX116 and AQ-RA741 and the M3-selective antagonists 4-DAMP and p-FHHSiD. The potency of these compounds was quantified by means of pA2 values. Atropine, a non-selective muscarinic antagonist, was used for comparison

Results:

The rank order of potency for the muscarinic receptor antagonists in preparations taken from SHR and WKY rats appears to be atropine>4-DAMP> p-FHHSiD>pirenzepine>AQ-RA 741 >AF-DX116. This rank order corresponds to that found in isolated conduit arteries

Conclusions:

The pA2 values for the various compounds were not significantly different in SHR and WKY rat preparations, indicating that the nature of this receptor is not influenced by hypertension. The high potency of the M3-selective drugs and the weak activity of pirenzepine and the M2-selective antagonists suggest a major role of M3-receptors in the cholinergic vasodilation in the perfused mesenteric vascular bed both in SHR and WKY rat preparations

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