ABSTRACT
Five substituted amides of ethylenediamines produced hypotension in dogs, which was not blocked by atropine, mepyramine and propranolol. The amides potentiated the pressor responses to Adr and NA and antagonised the depressor responses to Ach and histamine. The compounds also antagonised Ach-induced contractions on the frog rectus abdominis muscle and of carbachol on rat isolated colon suggesting d-tc and atropine-like actions respectively. Antihistaminic activity was observed on guinea pig isolated ileum as on dog blood pressure. Adr and NA-induced relaxation of rabbit isolated jejunum was potentiated. Finally Adr and NA-induced contractions of rat isolated seminal vesicle was antagonised.
Subject(s)
Amides/pharmacology , Animals , Blood Pressure/drug effects , Chemical Phenomena , Chemistry , Colon , Dogs , Ethylenediamines/pharmacology , Female , Guinea Pigs , Ileum , Jejunum , Male , Muscle Contraction/drug effects , Muscle, Smooth/drug effects , Muscles/drug effects , Rabbits , Rats , Seminal VesiclesABSTRACT
Substituted benzylamide derivatives of amino acylamide (compound A,B,C, & D) were found to be less potent local anaesthetics than lignocaine and procaine. However, the four compounds exhibited sedation without ptosis and reduced spontaneous locomotor activity better than methaqualone. Compound A alone antagonised methylamphetamine induced hypermotor activity. The test compounds potentiated hexobarbitone induced hypnosis. Three compounds antagonised calcium induced stoppage of isolated heart of frog. Except compound C all caused a transitory fall of blood pressure in dog which was not blocked either by atropine or propranolol. These compounds showed neuromuscular blockade and possessed slight analgesic activity but were devoid of anticonvulsant and tranquillizing activity. LD 50 values were calculated to be 164.1 +/- 23.0, 229.1 +/- 51.0, 181.6 +/- 28.18 and 416+/-38.2 mg/kg for compounds A,B,C & D respectively.