37762-06-4 Usage
Description
Zaprinast, a cGMP-specific phosphodiesterase inhibitor, is a yellow-orange crystalline powder that plays a crucial role in signal transduction and a wide range of cellular processes. It is derived from the compound used in the development of sildenafil (Viagra) and has the ability to moderately inhibit PDE5 and PDE6, as well as weakly inhibit PDE9, PDE10, and PDE11.
Uses
Used in Pharmaceutical Industry:
Zaprinast is used as a cGMP phosphodiesterase inhibitor for its vasodilating, relaxant, and diuretic effects. It enhances the vasodilatory effects of nitric oxide in various vascular tissues by prolonging the cGMP-mediated activation of cGMP-dependent protein kinase, making it potentially useful in treating hypertension and congestive heart failure.
Used in Reproductive Biology Research:
Zaprinast is used as an inhibitor in the meiosis of oocytes by germinal vesicle breakdown (GVBD) assay, helping researchers understand its effects on oocyte development and meiosis.
Used in Retinal Cell Research:
Zaprinast is used to test the inhibitory effect on retinal cells through immunohistochemistry, providing insights into its potential applications in ophthalmology and vision research.
Used in Signal Transduction Research:
Zaprinast is used as a research tool to study the activation of the rat and human G protein-coupled receptor, GPR35, with EC50 values of 16 nM and 0.84 μM, respectively, contributing to the understanding of signal transduction pathways and their role in various cellular processes.
Biological Activity
Phosphodiesterase inhibitor, selective for PDE6, 5, 11 and 9 (IC 50 values are 0.15, 0.76, 12.0 and 29.0 μ M respectively).
Biochem/physiol Actions
Zaprinast insubstantially inhibits phosphodiesterase 10 and 11 (PDE10 and PDE11). It also exhibits vasodilating effects.
in vitro
zaprinast is a pde5 and pde6 inhibitor with inhibiting pde9 at moderately high concentrations (29 mm) [1]. indeed, it showed that inhibition of cgmp hydrolysis by infusion of zaprinast increases the effect of anp on natriuresis with no causing deleterious drops in blood pressure. because it was known that anp receptors is localized within the glomerulus and inner medullary collecting ducts, to determine the cellular localization of pde9 enzyme in kidney will be interesting. [2]. the enzyme displayed a high specificity for cgmp with binding sites for cgmp, and a sensitivity to zaprinast similar to smooth muscle pde5, resulting in both enzymes were named cgmp-pde. however, retinal cgmp-pde was first distinguished as photoreceptor cgmp-pde with being specifically distributed in the retina and having a higher vmax and km values than other cgmp-pdes and being modulated by g protein. [3].
IC 50
0.15, 0.76, 12.0 and 29.0 μm for pde6, 5, 11 and 9 respectively.
references
[1] christensen and torphy (1994) isozyme-selective phosphodiesterase inhibitors as antiasthmatic agents. annu.rep.med.chem. 29 185.[2] soderling sh, bayuga sj, beavo ja. identification and characterization of a novel family of cyclic nucleotide phosphodiesterases. j biol chem. 1998 jun 19; 273(25):15553-8.[3]. lugnier c. cyclic nucleotide phosphodiesterase (pde) superfamily: a new target for the development of specific therapeutic agents. pharmacol ther. 2006 mar; 109 (3):366-98. epub 2005 aug 15.
Check Digit Verification of cas no
The CAS Registry Mumber 37762-06-4 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 3,7,7,6 and 2 respectively; the second part has 2 digits, 0 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 37762-06:
(7*3)+(6*7)+(5*7)+(4*6)+(3*2)+(2*0)+(1*6)=134
134 % 10 = 4
So 37762-06-4 is a valid CAS Registry Number.
InChI:InChI=1/C13H13N5O2/c1-2-7-20-9-6-4-3-5-8(9)11-14-12-10(13(19)15-11)16-18-17-12/h3-6H,2,7H2,1H3,(H2,14,15,16,17,18,19)
