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CGS 9343B
calmodulin antagonist; structure given in first source; RN given refers to parent cpd
Also Known As:
1,3-dihydro-1-(1-((4-methyl-4H,6H-pyrrolo(1,2a)(4,1)-benzoxazepin-4-yl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one; CGS 9343B maleate; CGS-9343B; KW-6517; Zy 17617B; Zy-17617B; zaldaride maleate
Networked:
16
relevant articles (
3
outcomes,
3
trials/studies)
Relationship Network
Bio-Agent Context: Research Results
Heterocyclic Compounds: 198
Fused-Ring Heterocyclic Compounds
2-Ring Heterocyclic Compounds
Benzimidazoles: 245
CGS 9343B: 16
Experts
1.
Aikawa, N
: 2 articles (04/2000 - 01/2000)
2.
Kobayashi, H
: 2 articles (04/2000 - 01/2000)
3.
Ohmori, K
: 2 articles (04/2000 - 01/2000)
4.
Horikoshi, K
: 1 article (04/2000)
5.
Maeda, H
: 1 article (04/2000)
Related Diseases
1.
Diarrhea
10/01/1989 - "
CGS 9343B was the most potent of these agents, eliminating diarrhea in 100% of mice at a dose of 1 mg/kg (p.o.).
"
04/01/1996 - "
DuPont and colleagues showed, for example, that oral therapy with zaldaride maleate relieves symptoms of disease and shortens the duration of diarrhea in travelers with ETEC-induced diarrhea.
"
04/01/2000 - "
Zaldaride maleate (ZAL), a calmodulin inhibitor, that ameliorates secretory diarrhea in rodents, has a racemic structure.
"
01/01/2000 - "
The amelioration of secretory diarrhea has been reported after the administration of zaldaride maleate (ZAL), a selective calmodulin inhibitor, to male rodents.
"
02/01/1998 - "
Effects of KW-5617 (zaldaride maleate), a potent and selective calmodulin inhibitor, on secretory diarrhea and on gastrointestinal propulsion in rats.
"
2.
Burns
01/01/1991 - "
Here we show that CGS 9343B, like other calmodulin antagonists reported previously, is most effective in treatment of burns.
"
01/01/1991 - "
3. As CGS 9343B is a more selective probe for calmodulin function than other inhibitors, the similarity of its effects on burns to that of other calmodulin antagonists, strongly suggest that their action on burns is mediated through calmodulin inhibition.
"
01/01/1991 - "
Effect of the calmodulin antagonist CGS 9343B on skin burns.
"
01/01/1991 - "
2. The effectiveness of CGS 9343B on skin burns was evaluated by electron microscopic studies, as well as by measurements of hemoglobin, ATP and enzymes which are markedly changed in the burned skin.
"
3.
Reperfusion Injury
02/01/1989 - "
Since this compound blocks calmodulin without inhibiting protein kinase C, the results of this study suggest that calmodulin-dependent kinase, rather than protein kinase C, is primarily involved in expressing calcium-overloaded cell exocytosis, and a specific calmodulin antagonist such as CGS 9343B can be used to salvage an ischemic heart from reperfusion injury.
"
4.
Visceral Pain
12/01/1999 - "
Using distention of the small intestine as a visceral pain model, we investigated the effect of zaldaride maleate (ZAL), a selective inhibitor of calmodulin, on the depressor response.
"
12/01/1999 - "
Effect of zaldaride maleate, an antidiarrheal compound, on visceral pain reflex induced by small intestinal distention in anesthetized rats.
"
5.
Pheochromocytoma
06/05/1992 - "
The calmodulin inhibitor 1,3-dihydro-1-[1-((4-methyl-4H,6H-pyrrolo[1,2-a]-[4,1]benzoxazepin - 4-yl)methyl)-4-piperidinyl]-2H-benzimidazol-2-one maleate (CGS 9343B) caused a reversible block of voltage-activated Ca2+, Na+, and K+ currents in differentiated rat pheochromocytoma (PC12) cells.
"
Related Drugs and Biologics
1.
Calmodulin (Calcium-Dependent Activator Protein)
2.
Loperamide (Imodium)
3.
Calcium
4.
Adenosine Triphosphate (ATP)
5.
Protein Kinase C
6.
Phosphotransferases (Kinase)
7.
Hemoglobins (Hemoglobin)
8.
Enzymes
9.
Antidiarrheals
10.
maleic acid (maleate)
Related Therapies and Procedures
1.
Therapeutics