Species-related specific differences in the pharmacological profile of vasopressin V1a receptors have been reported. Thus, the aim of the present study was to identify a vascular preparation of human origin expressing V1a receptors. Vasopressin was found to contract human gastric artery strips without endothelium with high affinity (pEC50 8.9). The maximal effect induced by vasopressin was inversely related to the diameter of the vessel. Oxytocin was found to contract the human gastric artery strips with low potency (pEC50 7.2). Contraction induced by vasopressin was competitively antagonized by the non peptide vasopressin receptor antagonists SR 49059 (pA2 9.2), OPC 21268 (pA2 6.2) and OPC 31260 (pA2 7.1). The order of potency of agonists (vasopressin > > oxytocin) and of antagonists (SR 49059 > > OPC 31260 > OPC 21268) indicate the contraction induced by vasopressin in the isolated human gastric artery is mediated by the V1a receptor type. The present data are similar to those obtained in different preparations expressing the native human V1a receptor as well as to those obtained in cell transfected with this receptor. The human gastric artery is a monoreceptor system of great utility for studying the effects of new drugs interacting with the human V1a receptor.
Pharmacological characterization of a vasopressin V1 receptor in the isolated human gastric artery
CALO', Girolamo;RIZZI, Anna;
1997
Abstract
Species-related specific differences in the pharmacological profile of vasopressin V1a receptors have been reported. Thus, the aim of the present study was to identify a vascular preparation of human origin expressing V1a receptors. Vasopressin was found to contract human gastric artery strips without endothelium with high affinity (pEC50 8.9). The maximal effect induced by vasopressin was inversely related to the diameter of the vessel. Oxytocin was found to contract the human gastric artery strips with low potency (pEC50 7.2). Contraction induced by vasopressin was competitively antagonized by the non peptide vasopressin receptor antagonists SR 49059 (pA2 9.2), OPC 21268 (pA2 6.2) and OPC 31260 (pA2 7.1). The order of potency of agonists (vasopressin > > oxytocin) and of antagonists (SR 49059 > > OPC 31260 > OPC 21268) indicate the contraction induced by vasopressin in the isolated human gastric artery is mediated by the V1a receptor type. The present data are similar to those obtained in different preparations expressing the native human V1a receptor as well as to those obtained in cell transfected with this receptor. The human gastric artery is a monoreceptor system of great utility for studying the effects of new drugs interacting with the human V1a receptor.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
