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Discovery of Potent, Selective, and Short-Acting Peptidic V2 Receptor Agonists.

Abstract：

:The vasopressin analogue desmopressin (desamino-d-arginine8 vasopressin, dDAVP, 1) is a potent vasopressin 2 (V2) receptor (V2R) agonist approved in many countries for the treatment of diabetes insipidus, primary nocturnal enuresis, nocturia, and coagulation disorders. Since 1 is primarily excreted via the kidneys, an age-related decline in kidney function leads to slower elimination, prolonged antidiuresis, and hyponatremia. In search of novel, potent, selective, and short-acting peptidic V2R agonists, we synthesized a series of C-terminally truncated analogues of [Val4]dDAVP, 2, modified in positions 2, 3, and 7 and/or at the disulfide bridge. The peptides were evaluated for in vitro potency at the human V2 receptor, selectivity versus the related receptors (human vasopressin 1a receptor, human vasopressin 1b receptor, and human oxytocin receptor), and pharmacokinetic profiles in rodents and other higher species. The truncated analogues show excellent potency at the V2R, increased systemic clearance, and shorter half-life in rats. Two compounds 19 (c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-Agm) and 38 (c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2) have been selected for clinical development for nocturia.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Wiśniewski K,Qi S,Kraus J,Ly B,Srinivasan K,Tariga H,Croston G,La E,Wiśniewska H,Ortiz C,Laporte R,Rivière PJ,Neyer G,Hargrove DM,Schteingart CD

doi

10.1021/acs.jmedchem.9b00132

subject

Has Abstract

pub_date

2019-05-23 00:00:00

pages

4991-5005

issue

10

eissn

0022-2623

issn

1520-4804

journal_volume

62

pub_type

杂志文章

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