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The antiulcer and antisecretory activity of WHR‐1370A 1‐n‐butoxy‐3‐(2,6 dimethylphenylcarbamoyl) guanidine hydrochloride
Author(s) -
Taylor J. A.,
Eash J. R.,
Nabi Mir G.
Publication year - 1982
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430020610
Subject(s) - chemistry , phentolamine , yohimbine , medicine , hydrochloride , methysergide , endocrinology , cysteamine , propranolol , pylorus , atropine , pharmacology , reserpine , stomach , biochemistry , antagonist , receptor
WHR‐1370A in the rat reduces volume (ED50 = 1.3 mg/kg p.o.) acidity (1.8 p.o.), and pepsin (2.8 p.o.) in the 4‐hr pylorus ligation model, delays gastric emptying (0.75 p.o.), and protects against the development of stress (18‐hr restraint)‐, indomethanic‐, aspirin‐, reserpine‐, and cysteamine‐induced ulcers (ED50s: 10.0 s.c., .65 p.o., 0.59 p.o., 3.0 p.o., and 8.0 s.c., respectively); also WHR‐1370A can completely suppress the cysteamine‐induced rise in serum gastrin. In the pylorus‐ligated rat, the activity of WHR‐1370A is not appreciably altered by methysergide, pimozide, propranolol, corynanthine, or phentolamine but is significantly and competitively antagonized by yohimbine. The pharmacological basis of WHR‐1370A probably can be attributed to an alpha‐2‐mediated inhibition of acetylcholine release at vagal nerve endings.