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
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
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).
Name | Type | Language | ||
---|---|---|---|---|
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English |
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
RA7HHG7F9H
Created by
admin on Sat Dec 16 05:34:49 GMT 2023 , Edited by admin on Sat Dec 16 05:34:49 GMT 2023
|
PRIMARY | |||
|
RA7HHG7F9H
Created by
admin on Sat Dec 16 05:34:49 GMT 2023 , Edited by admin on Sat Dec 16 05:34:49 GMT 2023
|
PRIMARY | |||
|
2257602
Created by
admin on Sat Dec 16 05:34:49 GMT 2023 , Edited by admin on Sat Dec 16 05:34:49 GMT 2023
|
PRIMARY | |||
|
730233-46-2
Created by
admin on Sat Dec 16 05:34:49 GMT 2023 , Edited by admin on Sat Dec 16 05:34:49 GMT 2023
|
PRIMARY | |||
|
38667
Created by
admin on Sat Dec 16 05:34:49 GMT 2023 , Edited by admin on Sat Dec 16 05:34:49 GMT 2023
|
PRIMARY | |||
|
DTXSID70223300
Created by
admin on Sat Dec 16 05:34:49 GMT 2023 , Edited by admin on Sat Dec 16 05:34:49 GMT 2023
|
PRIMARY |
ACTIVE MOIETY