CARDIOVASCULAR PROPERTIES OF THE NEW ANTIULCER DRUG YL)ETHYL]CARBAMOYL]METHYL]-AMINO-N-METHYLBENZAMIDE

Cardiovascular activities of 3-[[[2-(3,4-dimethoxyphenyl) ethyl]carbam oyl]methyl]-amino-N-methylbenzamide (DQ-2511, CAS 104775-36-2), an ant i-ulcer drug, were investigated in anesthetized dogs and conscious rat s. In anesthetized and laparotomized dogs, DQ-2511 at intravenous dose s of 5-50 mg/kg dose-relatedly induced an increase in celiac and mesen teric arterial blood flow, and a decrease in their resistance, whereas the drug had little or no effect on carotid and renal blood flow. DQ- 2511 increased cardiac contractility in anesthetized dogs at an intrav enous dose of 15 mg/kg. In addition to this effect, it produced an inc rease in respiratory rate, a decrease in blood pressure and a slight i ncrease in heart rate after dosing at 50 mg/kg. The drug had little or no effect on femoral blood flow and produced no significant changes i n the electrocardiogram. In conscious rats, blood flow in gastrointest inal organs was compared with flow in other organs using the microsphe re method. Blood flow in the stomach, duodenum, ileum, pancreas, splee n, and kidney tended to decrease in the vehicle-treated control group. DQ-2511, at an oral dose of 100 mg/kg, significantly increased bloodf low in the stomach, duodenum and spleen, and tended to increase flow i n the pancreas, testis and fat in comparison with the vehicle-treated control group. Bloodflow in the liver, heart and skeletal muscle tende d to decrease, whereas the other regional blood flows did not differ f rom those in the control group. DQ-2511 at this oral dose had little o r no effect on blood pressure, heart rate, cardiac output and total pe ripheral resistance in rats. In conclusion, DQ-2511 can be considered to selectively increase gastrointestinal blood flow rather than other regional bloodflows. This vasodilation may play an important role in t he anti-ulcer activity of this drug.