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Title: A V1-vascular vasopressin antagonist suitable for radioiodination and photoaffinity labeling

Journal Article · · American Journal of Hypertension; (USA)
DOI:https://doi.org/10.1093/ajh/3.6.471· OSTI ID:6644075
; ;  [1]
  1. University Hospital of Cleveland, O (USA)

We have previously characterized the V1-vascular arginine vasopressin (AVP) receptors of human platelets. We now report on a radiomonoiodinated and photoreactive V1-vascular AVP antagonist (V1-ag) to be used for the purification of human V1-vascular AVP receptors. The V1-ag, d(CH2)5Tyr(Me)Tyr(NH2)AVP was modified by radiomonoiodination of d(CH2)5-Tyr(Me)Tyr(NH2)AVP with the Iodogen technique, and derivatization of d(CH2)5Tyr(Me)Tyr(125I)(NH2)-AVP with the photoreactive crosslinker, N-hydroxysuccinimidyl-4-azidobenzoate (HSAB) (each step included HPLC purification). In competition experiments, the affinity of these V1-ag for the human platelet AVP receptors remained excellent. Irreversible photoaffinity labeling of the platelet V1-vascular AVP receptor was successfully achieved by UV lamp exposure (365 nm, 20 min). Thus, AzBz-d(CH2)5Tyr(Me)Tyr(125I)(NH2)AVP is a promising tool to use for the purification of human V1-vascular AVP receptors.

OSTI ID:
6644075
Journal Information:
American Journal of Hypertension; (USA), Vol. 3; ISSN 0895-7061
Country of Publication:
United States
Language:
English