RESUMEN
Five of the substituted ethylenediamine amides (LMG I to V) were tested for various CNS attributes and for acute toxicity (24 hr mortality). All compounds were potent analgesics in various animal tests, LMG V being most potent. All reduced spontaneous activity of mice and potentiated ether anaesthesia. However, CAR was not altered and anti-MES were not pronounced in rats. Compounds appear to have a wide safety margin considering ED50 and LD50 in mice.
Asunto(s)
Amidas/farmacología , Analgésicos/farmacología , Animales , Sistema Nervioso Central/efectos de los fármacos , Etilenodiaminas/farmacología , Femenino , Dosificación Letal Mediana , Masculino , Ratones , Actividad Motora/efectos de los fármacos , Ratas , Reflejo/efectos de los fármacosRESUMEN
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.
Asunto(s)
Amidas/farmacología , Animales , Presión Sanguínea/efectos de los fármacos , Fenómenos Químicos , Química , Colon , Perros , Etilenodiaminas/farmacología , Femenino , Cobayas , Íleon , Yeyuno , Masculino , Contracción Muscular/efectos de los fármacos , Músculo Liso/efectos de los fármacos , Músculos/efectos de los fármacos , Conejos , Ratas , Vesículas SeminalesRESUMEN
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.