GENERAL PHARMACOLOGICAL PROFILE OF THE NEW ANTIULCER DRUG YL)ETHYL]CARBAMOYL]METHYL]-AMINO-N-METHYLBENZAMIDE

Pharmacological properties of the anti-ulcer drug 3-[[[2-(3,4-dimethox yphenyl) ethyl] carbamoyl] methyl]-amino-N-methylbenzamide (DQ-2511, C AS 104775-36-2) on the central and autonomic nervous systems, smooth m uscle, gastrointestinal system, and other miscellaneous systems were i nvestigated 1. DQ-2511 showed little or no influence on general behavi or, spontaneous motor activity, hexobarbital sleeping time (mouse), co nditioned avoidance response (rat), body temperature (rabbit), EEG or spinal reflex (cat) after oral administration (300-1000 mg/kg) or intr avenous injection (15, 50 mg/kg). It also had no anticonvulsant or ana lgesic activities (mouse). 2. DQ-2511 had no influence on pupil size ( rabbit). It reduced or tended to reduce contractile responses of the n ictitating membrane induced by electrical stimulation of pre- and post -ganglionic sympathetic nerve (cat) at the highest dose. The drug inhi bited the pressor response to norepinephrine, but had little or no inh ibitory effect on the depressor response to acetylcholine at the highe st dose (dog). 3. DQ-2511 reduced contractile responses to nicotine, B aCl2, acetylcholine, histamine and serotonin (isolated guinea pig ileu m), to acetylcholine and histamine (trachea), and to norepinephrine (v as 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 5-5 0 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). 5. DQ-2 511 showed no activity on urine volume or urinary electrolyte excretio n (rat), and no local anesthetic activity (guinea pig) even at the hig hest dose. It produced a slight potentiation of skeletal muscle contra ctile response to direct (muscle) and nerve stimulation (rabbit), with potentiation of the response to nerve stimulation being somewhat larg er than that to muscle stimulation. DQ-2511 is considered to have no s ignificant general pharmacological activities, except on the gastroint estinal system.