[Effects of CN-100 (2-(10,11-dihydro-10-oxodibenzo [b,f] thiepin-2-yl) propionic acid) on cardiovascular and autonomic nervous function in the dog and guinea pig].
1) In pentobarbital-anesthetized dogs, intravenous administration of CN-100 at 40 mg/kg exhibited a transient hypotension, accompanied with a slight respiratory excitation and a temporal increase of heart rate followed by slight and gradual decrease at 20 and 40 mg/kg. 2) In isolated guinea pig atria, CN-100 (10(-4), 10(-5) g/ml) decreased the heart rate, without influencing the myocardial contraction. 3) In anesthetized dogs, the vertebral and carotid blood flow slightly and gradually increased at 5-20 mg/kg and decreased at 40 mg/kg. The drug at 20 mg/kg similarly increased the femoral flow. 4) In anesthetized dogs, CN-100 (40 mg/kg) slightly potentiated hypertensive responses to noradrenaline and adrenaline, without affecting heart rate responses to these amines. 5) In anesthetized dogs, CN-100 (40 mg/kg) scarcely had effect on the blood pressure rise and bradycardia induced by respective proximal and distal end stimulation of the severed vagus nerve, but enhanced the hypertension due to the carotid sinus reflex. CN-100 augmented the tachycardia elicited by pre- and postganglionic stellate stimulation in spinal dogs. 6) In isolated guinea pig trachea muscle, CN-100 (3 x 10(-6) g/ml) reduced the resting tone and relaxation response to noradrenaline, but slightly enhanced contractile responses to field stimulation and acetylcholine. 7) These results suggest that CN-100 exerts weak cardiovascular and autonomic nervous actions.
Kushiku
K
K
Department of Pharmacology, School of Medicine, Fukuoka University, Japan.
Abe
M
M
Morishita
H
H
Furukawa
T
T
D000818:Animals; D001341:Autonomic Nervous System / Q000187:drug effects*; D001582:Benzothiepins / Q000494:pharmacology*; D002395:Catecholamines / Q000494:pharmacology; D004285:Dogs; D004347:Drug Interactions; D005260:Female; D006168:Guinea Pigs; D006439:Hemodynamics / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009200:Myocardial Contraction / Q000187:drug effects*; D012119:Respiration / Q000187:drug effects*; D014132:Trachea / Q000187:drug effects
D001582:Benzothiepins; D002395:Catecholamines; C051758:CN 100