On the long acting gastric antisecretory activity of LM 24056 a non H2 antagonist
| Autor: | G. Le Fur, C. Jozefczak, Andre Uzan, J. Rataud, J. Mizoule, D. Quarteronet |
|---|---|
| Rok vydání: | 1982 |
| Předmět: |
medicine.medical_specialty
Carbachol medicine.medical_treatment Metabolite Pharmacology General Biochemistry Genetics and Molecular Biology H2 antagonist Gastric Acid chemistry.chemical_compound Mice Dogs Phenothiazines Internal medicine Muscarinic acetylcholine receptor Gastrins medicine Animals General Pharmacology Toxicology and Pharmaceutics Gastrin Chemistry Stomach General Medicine Desmethyl Receptors Muscarinic Rats Pentagastrin Kinetics Endocrinology Food Female Histamine medicine.drug |
| Zdroj: | Life sciences. 31(14) |
| ISSN: | 0024-3205 |
| Popis: | LM 24056, a phenothiazine derivative with no central effects, can be classified as a non anti H 2 antisecretory agent with a long duration of action. Its activity was demonstrated orally at low dose in pentagastrin stimulated Shay rat and in Heidenhain pouch in dog against gastrin, pentagastrin, carbachol and test meal. LM 24056 was inactive in histamine induced secretion. LM 24056 possesses very weak affinity to muscarinic receptors in vitro and in vivo. It has negligible anticholinergic properties in rats and mice at the peripheral level but no effect at the central level. The long lasting antisecretory action of LM 24056 may be supported by the persistent presence in plasma of a desmethyl metabolite at higher concentrations tham that of LM 24056 at any time. Contrary to LM 24056 sulfoxide and LM 24056 sulfone, desmethyl LM 24056 is a more potent antisecretory drug than LM 24056. Desmethyl LM 24056 possesses more marked affinity to peripheral muscarinic receptor than LM 24056. As the administration of therapeutic doses of LM 24056 was not followed by anticholinergic side-effects, it may be suggested that LM 24056 activity is related to a “prodrug like effect”. Finally the activity of LM 24056 may be related to LM 24056 itself and/or a desmethyl metabolite. |
| Databáze: | OpenAIRE |
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