Levocabastine: pharmacological profile of a highly effective inhibitor of allergic reactions.
Levocabastine, selected from a series of cyclohexylpiperidine derivatives protects rats from compound 48/80-induced anaphylactic shock for at least 16 h at the oral dose of 0.0015 mg/kg. At the same dose histamine skin reactions and at slightly higher doses passive cutaneous anaphylactic reactions are inhibited. Blockade of passive cutaneous anaphylactic reactions is obtained with levocabastine, despite absence of peripheral serotonin antagonism and any other known non-specific action that may facilitate inhibition of passive anaphylaxis. In dogs allergic reactions are inhibited at oral doses 40 times lower than ketotifen. In guinea-pigs orally and topically administered levocabastine are remarkably effective against allergic conjunctivitis.
Awouters
F
F
Janssen Research Foundation, Beerse, Belgium.
Niemegeers
C J
CJ
Jansen
T
T
Megens
A A
AA
Janssen
P A
PA
D000707:Anaphylaxis / Q000139:chemically induced / Q000517:prevention & control; D000818:Animals; D001200:Ascaris / Q000276:immunology; D003233:Conjunctivitis, Allergic / Q000188:drug therapy; D004285:Dogs; D006168:Guinea Pigs; D006632:Histamine; D006634:Histamine H1 Antagonists / Q000494:pharmacology / Q000627:therapeutic use*; D006967:Hypersensitivity / Q000188:drug therapy* / Q000209:etiology / Q000517:prevention & control; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D010880:Piperidines / Q000494:pharmacology / Q000627:therapeutic use*; D051381:Rats; D003189:p-Methoxy-N-methylphenethylamine
D006634:Histamine H1 Antagonists; D010880:Piperidines; D003189:p-Methoxy-N-methylphenethylamine; D006632:Histamine; C047340:levocabastine