title: Radioligand binding studies reveal marked species differences in the vasopressin V1 receptor of rat, rhesus and human tissues.
abstract: The [3H]arginine-vasopressin ([3H]AVP) binding site in rat, rhesus and human liver and nonpregnant human uterus was characterized and contrasted. [3H]AVP bound with high affinity (Ki values, 0.2-0.6 nM) to preparations of all tissues studied. Competition binding studies using a series of compounds from three structural classes indicate a marked species difference between the rat and primate liver AVP-V1 site. This site in rhesus and human liver however, is essentially identical, indicating that the rhesus liver is an appropriate surrogate for human tissue. These studies also indicate that the AVP-V1 site of nonpregnant human uterus and human liver is equivalent.
authors.affiliation: Department of New Lead Pharmacology, Merck Sharp & Dohme Research Laboratories, West Point, PA 19486.
authors.forename: D J
authors.initials: DJ
authors.lastname: Pettibone
authors.forename: M T
authors.initials: MT
authors.lastname: Kishel
authors.forename: C J
authors.initials: CJ
authors.lastname: Woyden
authors.forename: B V
authors.initials: BV
authors.lastname: Clineschmidt
authors.forename: M G
authors.initials: MG
authors.lastname: Bock
authors.forename: R M
authors.initials: RM
authors.lastname: Freidinger
authors.forename: D F
authors.initials: DF
authors.lastname: Veber
authors.forename: P D
authors.initials: PD
authors.lastname: Williams
mesh_terms: D000818:Animals; D001127:Arginine Vasopressin / Q000037:antagonists & inhibitors / Q000378:metabolism*; D001665:Binding Sites; D001667:Binding, Competitive; D005260:Female; D006801:Humans; D008099:Liver / Q000378:metabolism*; D008253:Macaca mulatta; D008297:Male; D009842:Oligopeptides / Q000378:metabolism; D011869:Radioligand Assay; D051381:Rats; D011919:Rats, Inbred Strains; D011945:Receptors, Angiotensin / Q000378:metabolism*; D017483:Receptors, Vasopressin; D013045:Species Specificity; D014599:Uterus / Q000378:metabolism*
chemical_list: D009842:Oligopeptides; D011945:Receptors, Angiotensin; D017483:Receptors, Vasopressin; D001127:Arginine Vasopressin