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iso-PPADS tetrasodium salt Sale

目录号 : GC10990

P2 purinoceptors antagonist, specific

iso-PPADS tetrasodium salt Chemical Structure

Cas No.:207572-67-6

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产品描述

Iso-PPADS tetrasodium salt is a specific P2 purinoceptors antagonist [3].
P2 purinoceptors mediate the actions of adenosine 5'-tri- phosphate (ATP) on many physiological systems including most vascular and visceral smooth muscles and certain neur- ones in the peripheral and central nervous systems
IsoPPADS (10 uM) depressed alpha, beta-Me-ATP-evoked depolarizations but did not alter depolarizations evoked by UTP. So it is concluded that IsoPPADS is antagonist at P2x-purinoceptor but not at the receptor that mediate UTP-evoked depolarization of the rat superior cervical ganglion [1]. In functional studies, iso-PPADS identified two populations of [3H]alpha,beta-meATP binding sites, 26.4% of these having low affinity (pKi of 4.4 +/- 0.2), and 73.6% having high affinity (pKi of 6.5 +/- 0.02) for iso-PPADS [2]. Iso-PPADS (1 X 10-6 -1 X 10-5 M) produced a concentration-related depression in the maxima of the concentration-effect curves to alpha,beta-methylene ATP.  The antagonistic effect of iso-PPADS (1 x 10-5 M) was partially attenuated by suramin (1 x 10-4 M) and this interaction reflects a slow dissociation of iso-PPADS from the receptor with which suramin and alpha, beta-methylene ATP interact [3].
Reference:
[1]. Connolly GP. Differentiation by pyridoxal 5-phosphate, PPADS and isoPPADS between responses mediated by UTP and those evoked by α, β-methylene-ATP on rat sympathetic ganglia. Br J Pharmacol, 1995, 114(3): 727-731.
[2]. Khakh BS, Michel A, Humphrey PP. Estimates of antagonist affinities at P2X purinoceptors in rat vas deferens. Eur J Pharmacol, 1994, 263(3): 301-309.
[3]. Trezise DJ, Kennedy I, Humphrey PP. The use of antagonists to characterize the receptors mediating depolarization of the rat isolated vagus nerve by α,β-methylene adenosine 5'-triphosphate. Br J Pharmacol, 1994, 112(1): 282-288.

Chemical Properties

Cas No. 207572-67-6 SDF
化学名 sodium (Z)-2-(2-(4-formyl-6-methyl-5-oxo-3-((phosphonatooxy)methyl)pyridin-2(5H)-ylidene)hydrazinyl)benzene-1,4-disulfonate
Canonical SMILES [O-]S(=O)(C(C(N/N=C(C(COP([O-])([O-])=O)=C1C=O)\N=C(C)C1=O)=C2)=CC=C2S([O-])(=O)=O)=O.[Na+].[Na+].[Na+].[Na+]
分子式 C14H10N3Na4O12PS2 分子量 599.3
溶解度 <59.93mg/ml in Water 储存条件 Desiccate at -20°C
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1 mM 1.6686 mL 8.3431 mL 16.6861 mL
5 mM 0.3337 mL 1.6686 mL 3.3372 mL
10 mM 0.1669 mL 0.8343 mL 1.6686 mL
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