General pharmacological profile of the new anti-ulcer drug 3-[[[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl]methyl]-amino-N -methylbenzamide.
Pharmacological properties of the anti-ulcer drug 3-[[[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl] methyl]-amino-N-methylbenzamide (DQ-2511, CAS 104775-36-2) on the central and autonomic nervous systems, smooth muscle, gastrointestinal system, and other miscellaneous systems were investigated. 1. DQ-2511 showed little or no influence on general behavior, spontaneous motor activity, hexobarbital sleeping time (mouse), conditioned avoidance response (rat), body temperature (rabbit), EEG or spinal reflex (cat) after oral administration (300-1000 mg/kg) or intravenous injection (15, 50 mg/kg). It also had no anticonvulsant or analgesic activities (mouse). 2. DQ-2511 had no influence on pupil size (rabbit). It reduced or tended to reduce contractile responses of the nictitating membrane induced by electrical stimulation of pre- and post-ganglionic sympathetic nerve (cat) at the highest dose. The drug inhibited the pressor response to norepinephrine, but had little or no inhibitory effect on the depressor response to acetylcholine at the highest dose (dog). 3. DQ-2511 reduced contractile responses to nicotine, BaCl2, acetylcholine, histamine and serotonin (isolated guinea pig ileum), to acetylcholine and histamine (trachea), and to norepinephrine (vas deferens) at high concentrations. It also inhibited spontaneous and oxytocin-induced motility (isolated rat uterus). 4. DQ-2511 decreased gastric motility in a dose-related manner at intravenous doses of 5-50 mg/kg (dog). It also reduced gastric emptying rate at oral doses of 100-1000 mg/kg, and gastric secretion at intraperitoneal doses of 100-300 mg/kg (rat). On the other hand, it induced no definite changes in intestinal motility (dog) or gastrointestinal transit (mouse).(ABSTRACT TRUNCATED AT 250 WORDS)
Hirohashi
M
M
Developmental Research Laboratories, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
Takasuna
K
K
Kasai
Y
Y
Usui
C
C
Tamura
K
K
Kojima
H
H
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology; D000897:Anti-Ulcer Agents / Q000494:pharmacology*; D001341:Autonomic Nervous System / Q000187:drug effects; D001549:Benzamides / Q000494:pharmacology*; D002415:Cats; D002490:Central Nervous System / Q000187:drug effects; D004064:Digestive System / Q000187:drug effects; D004285:Dogs; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D011247:Pregnancy; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D014563:Urodynamics / Q000187:drug effects
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000897:Anti-Ulcer Agents; D001549:Benzamides; C058308:ecabapide