Details
Stereochemistry | ACHIRAL |
Molecular Formula | C15H11Cl2N2 |
Molecular Weight | 290.167 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 1 |
SHOW SMILES / InChI
SMILES
ClC1=CC=C(NC2=CC=[N+]3C=CC=CC3=C2)C=C1Cl
InChI
InChIKey=MTFYFZDTISVQRR-UHFFFAOYSA-O
InChI=1S/C15H10Cl2N2/c16-14-5-4-11(10-15(14)17)18-12-6-8-19-7-2-1-3-13(19)9-12/h1-10H/p+1
Molecular Formula | C15H10Cl2N2 |
Molecular Weight | 289.159 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 1 |
Optical Activity | NONE |
Nolinium bromide (NB) is a nonanticholinergic, gastric acid antisecretory agent and a gastrointestinal tract antispasmodic agent. The gastrointestinal antispasmodic action of NB has been demonstrated in a variety of test systems. The compound inhibited electrically induced contractions of rabbit ileum and nicotine-induced contractions of rat ileum in vitro, gastric emptying in fasted rats, and intestinal transport of a charcoal meal in mice. In the anesthetized dog, NB antagonized colonic contractions induced by acetylcholine, histamine, serotonin, and pelvic nerve stimulation, and duodenal contractions due to vagal stimulation and acetylcholine. In the unanesthetized dog, feeding induced colonic and duodenal motilities were inhibited by NB. The antisecretory action of NB may involve inhibition of enzymes of gastric acid secretion, specifically histamine-stimulated adenylate cyclase and potassium-stimulated ATPase. NB has no direct histamine-H2 receptor blocking properties. Nolinium bromide inhibits in a dose-dependent manner both the gastric H+, K+-ATPase activity and H+ uptake ability of the gastric microsomes. Increasing concentrations of K+ could reverse the nolinium bromide inhibition of both the H+, K+-ATPase activity and vesicular H+ transport. Nolinium bromide interferes primarily with the K+-dependent phosphatase step and thereby reduces the turnover of the enzyme. The drug acts as a K+ antagonist in the gastric H+ +K+-dependent ATPase reaction.
Approval Year
PubMed
Title | Date | PubMed |
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Inhibition of histamine-sensitive adenylate cyclase from the guinea pig gastric mucosa by nolinium bromide. | 1979 |
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Effect of nolinium bromide, cimetidine, and oxyphencyclimine on gastric hypersecretion induced by some secretagogues in the rat. | 1980 Sep |
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Mechanism of gastric antisecretory effects of nolinium bromide. | 1983 Oct |
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Effect of nolinium bromide on vascular smooth muscle. | 1984 Sep |
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/6463055
Nolinium bromide (50-200 uM) was a reversible, insurmountable inhibitor of contractions induced by Ca2+ (in 40 mM KC1 depolarizing medium) and norepinephrine, with IC50 values of 96 and 118 uM, respectively, for suppression of maximum contractile force. Contractions in response to Asn1Val5-angiotensin II in both 2.5 mM Ca2+ and 0 mM Ca2+ medium were also inhibited (IC50 value = 110 uM under both conditions).
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 05:34:49 GMT 2023
by
admin
on
Sat Dec 16 05:34:49 GMT 2023
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Record UNII |
RA7HHG7F9H
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Record Status |
Validated (UNII)
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Record Version |
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-
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RA7HHG7F9H
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2257602
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730233-46-2
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38667
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DTXSID70223300
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