NF 023 - CAS 104869-31-0
Category: Inhibitor
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Molecular Formula:
C35H20N4Na6O21S6
Molecular Weight:
1162.86
COA:
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Targets:
P2X Receptor
Description:
NF 023 is a subtype-selective P2X1 receptor antagonist with IC50 value of 0.21μM for human P2X1.
Purity:
≥98% by HPLC
Synonyms:
NF 023; NF023; NF-023; 8,8'-[carbonylbis(imino-3,1-phenylenecarbonylimino)]bis-1,3,5-naphthalene-trisulphonic acid, hexasodium salt
MSDS:
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InChIKey:
FMQURVHYTBGYSQ-UHFFFAOYSA-H
InChI:
InChI=1S/C35H26N4O21S6.6Na/c40-33(38-25-7-9-27(63(49,50)51)23-13-21(61(43,44)45)15-29(31(23)25)65(55,56)57)17-3-1-5-19(11-17)36-35(42)37-20-6-2-4-18(12-20)34(41)39-26-8-10-28(64(52,53)54)24-14-22(62(46,47)48)16-30(32(24)26)66(58,59)60;;;;;;/h1-16H,(H,38,40)(H,39,41)(H2,36,37,42)(H,43,44,45)(H,46,47,48)(H,49,50,51)(H,52,53,54)(H,55,56,57)(H,58,59,60);;;;;;/q;6*+1/p-6
Canonical SMILES:
C1=CC(=CC(=C1)NC(=O)NC2=CC=CC(=C2)C(=O)NC3=C4C(=CC(=CC4=C(C=C3)S(=O)(=O)[O-])S(=O)(=O)[O-])S(=O)(=O)[O-])C(=O)NC5=C6C(=CC(=CC6=C(C=C5)S(=O)(=O)[O-])S(=O)(=O)[O-])S(=O)(=O)[O-].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]
1.Purinergic and nitrergic neuromuscular transmission mediates spontaneous neuronal activity in the rat colon.
Gil V;Gallego D;Grasa L;Martín MT;Jiménez M Am J Physiol Gastrointest Liver Physiol. 2010 Jul;299(1):G158-69. doi: 10.1152/ajpgi.00448.2009. Epub 2010 Apr 15.
Nitric oxide (NO) and ATP mediate smooth muscle relaxation in the gastrointestinal tract. However, the involvement of these neurotransmitters in spontaneous neuronal activity is unknown. The aim of the present work was to study spontaneous neuromuscular transmission in the rat midcolon. Microelectrode experiments were performed under constant stretch both in circular and longitudinal directions. Spontaneous inhibitory junction potentials (sIJP) were recorded. Tetrodotoxin (1 microM) and apamin (1 microM) depolarized smooth muscle cells and inhibited sIJP. N(omega)-nitro-l-arginine (l-NNA, 1 mM) depolarized smooth muscle cells but did not modify sIJP. In contrast, the P2Y(1) antagonist MRS-2500 (1 microM) did not modify the resting membrane potential (RMP) but reduced sIJP (IC(50) = 3.1 nM). Hexamethonium (200 microM), NF-023 (10 microM), and ondansetron (1 microM) did not modify RMP and sIJP. These results correlate with in vitro (muscle bath) and in vivo (strain gauges) data where l-NNA but not MRS-2500 induced a sustained increase of spontaneous motility. We concluded that, in the rat colon, inhibitory neurons regulate smooth muscle RMP and cause sIJP. In vitro, the release of inhibitory neurotransmitters is independent of nicotinic, P2X, and 5-hydroxytryptamine type 3 receptors.
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CAS 104869-31-0 NF 023

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