CLONING, FUNCTIONAL EXPRESSION AND TISSUE DISTRIBUTION OF HUMAN CDNA FOR THE VASCULAR-TYPE VASOPRESSIN RECEPTOR

We have cloned a human vasopressin receptor from human mesenteric artery using RACE (Rapid Amplification of cDNA Ends) methods. The deduced amino acid sequence of the clone (HV RACE) encodes a protein of 418 amino acids that showed a strong sequence homology to the previously cloned rat V-1A vasopressin receptor. The [H-3] arginine vasopressin (AVP) binding to HV-RACE expressed in COS-7 cells was potently inhibited by AVP (K-i = 2.9 nM). Interestingly, a new non-peptide ''V-1-selective'' antagonist OPC-21268 exhibited markedly higher affinity for rat V-1A receptor (K-i = 57 nM) rather than for HV-RACE (K-i = 56 mu M). With the reverse-transcription polymerase chain reaction assay, we observed a large amount of HV-RACE transcripts in the mesenteric artery, while a small amount in a variety of other tissues. The data show that the clone HV-RACE encodes a human vascular-type vasopressin receptor cDNA. (C) 1994 Academic Press, Inc.