Immunopharmacological studies on mydocalm and related compounds as an antagonist of slow reacting substance of anaphylaxis (SRS-A).
The antagonistic effect of 2,4'-dimethyl-3-piperidino propiophenone hydrochloride (Mydocalm) and its 15 derivatives against the activity of slow reacting substance of anaphylaxis (SRS-A) were examined in vitro. Mydocalm, 2-methyl-3-piperidino-beta-propionaphthone hydrochloride (As-5) and 2,3',4'-trimethyl-3 piperidinopropiophenone hydrochloride (As-14) were found to be potent antagonists to SRS-A. The above three compounds inhibited homologous passive cutaneous anaphylaxis (PCA) in rats and guinea pigs but not heterologous PCA in guinea pigs. As-5 inhibited the release of histamine from and the degranulation of rat mesenterium mast cells. As-14 also showed the inhibition of the degranulation. Mydocalm, however, showed no inhibition of these reactions. Experimental asthma in guinea pigs which were passively sensitized with guinea pig immunoglobulin E antibody was significantly inhibited by p.o. administration of Mydocalm, As-5 or As-14 respectively.
D000818:Animals; D001249:Asthma / Q000139:chemically induced; D003594:Cytoplasmic Granules / Q000187:drug effects; D005260:Female; D006168:Guinea Pigs; D006636:Histamine Release / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D011427:Propiophenones / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013189:SRS-A / Q000037:antagonists & inhibitors*; D013997:Time Factors; D014049:Tolperisone / Q000494:pharmacology*
D011427:Propiophenones; D013189:SRS-A; D014049:Tolperisone