Preparation and evaluation of a soluble derivative of the antiallergic compound trans-2, 3b, 4, 5, 7, 8b, 9, 10-octahydronaphtho [1, 2-c:5, 6-c'] dipyrazole (LC-6).
In the present report we describe the preparation of LC-6.2HCl, a soluble derivative of the synthetic bispyrazole LC-6. Because the latter was practically insoluble in aqueous and organic media, experiments which indicated that it had antiallergic activity were confined to in vivo studies following its oral administration. The availability of soluble LC-6.2HCl made it possible to administer the drug i.v. or i.p. Through these routes it exhibited greater antiallergic activity than by the oral route, as judged by lower ID50's and by the achievement of 100% PCA inhibition. The latter result had not previously been attained orally with the base. Furthermore, when injected i.v. or i.p. LC-6.2HCl showed prolonged inhibitory activity, a valuable attribute of the parent compound. The in vivo activity of the soluble salt, which we describe, further establishes the potential therapeutic value of the drug.
Hurtado
I
I
Urbina
C
C
Suárez
C
C
Beyer
B
B
Magro
A M
AM
D000284:Administration, Oral; D000818:Animals; D006634:Histamine H1 Antagonists / Q000494:pharmacology*; D006863:Hydrogen-Ion Concentration; D007274:Injections, Intraperitoneal; D007275:Injections, Intravenous; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D011720:Pyrazoles / Q000008:administration & dosage / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D012995:Solubility; D013997:Time Factors
D006634:Histamine H1 Antagonists; D011720:Pyrazoles; C016885:LC 6