Sedative action of some substituted benzylamides.
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.
D000577:Amides / Q000494:pharmacology*; D000779:Anesthetics, Local; D000818:Animals; D001001:Anura; D001593:Benzyl Compounds / Q000494:pharmacology*; D001794:Blood Pressure / Q000187:drug effects; D003864:Depression, Chemical; D004285:Dogs; D005260:Female; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006993:Hypnotics and Sedatives; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009132:Muscles / Q000187:drug effects; D011817:Rabbits; D051381:Rats
D000577:Amides; D000779:Anesthetics, Local; D001593:Benzyl Compounds; D006993:Hypnotics and Sedatives