(Arg6,β-cyclohexyl-Ala8,D-Tic16,Arg17,Cys18)-Atrial Natriuretic Factor (6-18) amide (mouse, rabbit, rat) trifluoroacetate salt

Names

[ Name ]:
(Arg6,β-cyclohexyl-Ala8,D-Tic16,Arg17,Cys18)-Atrial Natriuretic Factor (6-18) amide (mouse, rabbit, rat) trifluoroacetate salt

[Synonym ]:
(Arg6,β-cyclohexyl-Ala8,D-Tic16,Arg17,Cys18)-Atrial Natriuretic Factor (6-18) amide (mouse, rabbit, rat)

Biological Activity

[Description]:

A 71915 is a highly potent and competitive natriuretic peptide receptor A (ANP, NPRA) antagonist (pKi= 9.18). A 71915 displaces [125I]ANP dose dependently, with a Ki of 0.65 nM. A71915( pA2= 9.48) against rat ANP-induced cGMP production in NB-OK-1 cells[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Others >> Others

[Target]

A 71915 is a highly potent and competitive natriuretic peptide receptor A (ANP, NPRA) antagonist, with a pKi of 9.18.

[In Vitro]

A 71915 combines to Neuroblastoma NB-OK-1 cells, is used in the Cyclic GMP assay. A 71915 shifts the ANP dose-response curve of cyclic GMP production to the right[1].

[In Vivo]

A 71915 (5 μl; i.m.; 25-30 g male CD-1 mice) affects BNP (1 nmol)- and GRP (0.1 nmol)-induced scratching[2]. A 71915 (30 μg/ kg/ day) inhibits NS-398 on blood pressure decreased[3]. Animal Model: Rat (Male Sprague-Dawley); weighing 150-180 g[3] Dosage: 30 μg/kg/day; infused for 3 weeks Administration: via a mini-osmotic pump Result: The inhibitory effect of NS-398 on blood pressure was attenuated by the pretreatment with A 71915 (30 μg/kg/day).

[References]

[1]. Delporte C, et al. Discovery of a potent atrial natriuretic peptide antagonist for ANPA receptors in the human neuroblastoma NB-OK-1 cell line. Eur J Pharmacol. 1992;224(2-3):183-188.

[2]. Kiguchi N, et al. Spinal Functions of B-Type Natriuretic Peptide, Gastrin-Releasing Peptide, and Their Cognate Receptors for Regulating Itch in Mice.

[3]. Park BM, et al. Attenuation of renovascular hypertension by cyclooxygenase-2 inhibitor partly through ANP release. Peptides. 2015;69:1-8.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C₆₉H₁₁₆N₂₆O₁₅S₂

[ Molecular Weight ]:
1613.974

[ Exact Mass ]:
1612.855

[ LogP ]:
-5.73

[ Index of Refraction ]:
1.698

Related Compounds

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