Cardiovascular properties of the new anti-ulcer drug 3-[[[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl]methyl]-amino-N- methylbenzamide.
Cardiovascular activities of 3-[[[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl]methyl]-amino-N- methylbenzamide (DQ-2511, CAS 104775-36-2), an anti-ulcer drug, were investigated in anesthetized dogs and conscious rats. In anesthetized and laparotomized dogs, DQ-2511 at intravenous doses of 5-50 mg/kg dose-relatedly induced an increase in celiac and mesenteric 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 intravenous dose of 15 mg/kg. In addition to this effect, it produced an increase in respiratory rate, a decrease in blood pressure and a slight increase 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 in the electrocardiogram. In conscious rats, blood flow in gastrointestinal organs was compared with flow in other organs using the microsphere method. Blood flow in the stomach, duodenum, ileum, pancreas, spleen, and kidney tended to decrease in the vehicle-treated control group. DQ-2511, at an oral dose of 100 mg/kg, significantly increased blood flow in the stomach, duodenum and spleen, and tended to increase flow in the pancreas, testis and fat in comparison with the vehicle-treated control group. Blood flow in the liver, heart and skeletal muscle tended to decrease, whereas the other regional blood flows did not differ from those in the control group. DQ-2511 at this oral dose had little or no effect on blood pressure, heart rate, cardiac output and total peripheral resistance in rats.(ABSTRACT TRUNCATED AT 250 WORDS)
Hirohashi
M
M
Developmental Research Laboratories, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
Takasuna
K
K
Asano
M
M
Ryokawa
Y
Y
Tamura
K
K
D000758:Anesthesia; D000818:Animals; D000897:Anti-Ulcer Agents / Q000494:pharmacology*; D001549:Benzamides / Q000494:pharmacology*; D004064:Digestive System / Q000098:blood supply* / Q000187:drug effects; D004285:Dogs; D004562:Electrocardiography / Q000187:drug effects; D005260:Female; D006439:Hemodynamics / Q000187:drug effects*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D012039:Regional Blood Flow / Q000187:drug effects; D012079:Renal Circulation / Q000187:drug effects; D013152:Splanchnic Circulation / Q000187:drug effects
D000897:Anti-Ulcer Agents; D001549:Benzamides; C058308:ecabapide