Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:4.6.1.2 (guanylate cyclase)
 8,497 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The effect of N-(omega-aminoalkyl) derivatives of naphthalene-1-sulfamide on the activity of soluble guanylate cyclase and on human platelet aggregation at the first (reversible) step of the guanylate cyclase reaction was studied. Low (approximately 10(-7)-10(-6) M) concentrations of the above compounds were shown to stimulate the guanylate cyclase activity; some derivatives caused simultaneous inhibition of platelet aggregation induced by ADP. Some fragments of the chemical structure of the molecules responsible for the enzyme activity regulation in the tested systems were identified. The naphthalene-1-sulfamide derivatives carrying 6-aminohexyl or 8-amino-octyl groups of the sulfamide substituent as well as chlorine atom at positions 4 or 5 of the naphthalene ring appeared to be the most potent activators of platelet guanylate cyclase and inhibitors of platelet aggregation at the reversible step of the enzymatic reaction.
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PMID:[Effect of N-(6-aminohexyl)-5-chloronaphthalene-1-sulfamide (W-7) and its analogs on the activity of soluble guanylate cyclase and on human platelet aggregation]. 198 51

Chronic constipation is a common health problem that significantly affects the quality of life of patients and impacts in terms of costs; current treatments based on fiber and laxatives cause dissatisfaction to doctors and patients in more than half of the cases. New drugs are now available or in very advanced stages of research, with different and innovative mechanisms of action as prucalopride, lubiprostone, and linaclotide. Prucalopride an enterokinetic, is a selective high-affinity 5-hydroxytryptamine (5-HT)4 receptor agonist of serotonin that increases the peristaltic reflex and the colonic contractions; lubiprostone, a type 2 chlorine channel activator, or linaclotide, a guanylate cyclase-C agonist of enterocytes, both prosecretory agents, stimulate the secretion of fluid within the intestinal lumen. In general, these promising drugs have proven efficacy and safety as a specific therapeutic option in patients with chronic constipation. Yet the solution might not be sufficient for everybody and still without the ideal drug that might be useful in all cases, the pharmacological revolution for colonic motility disorders has arrived.
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PMID:Novel pharmacological therapies for management of chronic constipation. 2417 77

Constipation affects 15-25% of people. Its mechanisms are various. There are constipations due to intestinal dyskinesia (functional constipation, irritated bowel syndrome), slow transit (colonic inertia), and muscular apparatus discoordination ensuring defecation (dyssynergic defecation). The treatment of different types of constipation uses prokinetics (type 4 serotonin receptor agonists, chlorine channels activators and guanylate cyclase C channel activators) or spasmolytics, among which pinaverium bromide (dicetel) has demonstrated its high efficacy. Biofeedback therapy or surgical techniques may be used. There is a need to prescribe laxatives in any type of constipation. A pathogenetic approach to treating constipation is most efficient. The paper characterizes stimulant, osmotic, volume, and emollient laxatives and agents stimulating the urge to defecate. It also gives the data of meta-analyses evaluating the efficacy of different drug groups. Particular emphasis is laid of the effect of lactulose and its first preparation--duphalac.
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PMID:[Pathogenetic approaches to treating constipations]. 2530 54