iso-PPADS tetrasodium salt
目录号 : GC10990P2 purinoceptors antagonist, specific
Cas No.:207572-67-6
Sample solution is provided at 25 µL, 10mM.
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.
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 mg | 5 mg | 10 mg | |
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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% DMSO % % Tween 80 % saline | ||||||||||
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2.
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- Purity: >98.00%
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