5463. Levocabastine

Nomenclature

CAS number: 79516-68-0
[3S-[1(cis),3α,4β]]-1-[4-Cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenyl-4-piperidinecarboxylic acid; ()-trans-1-[cis-4-cyano-4-(p-fluorophenyl)cyclohexyl]-3-methyl-4-phenylisonipecotic acid; ()-cabastine.
C26H29FN2O2; mol wt 420.52.
C 74.26%, H 6.95%, F 4.52%, N 6.66%, O 7.61%.

Description and references

Histamine H1-receptor antagonist. Prepn: R. Stokbroekx et al., EP 34415; eidem, US 4369184 (1981, 1983 both to Janssen); and pharmacology: R. A. Stokbroekx et al., Drug Dev. Res. 8, 87 (1986). Pharmacology: K. Tasaka et al., Arzneim.-Forsch. 40, 1295 (1990). Clinical pharmacology: N. Rombaut et al., Ann. Allergy 67, 75 (1991). Clinical trial in children with allergic conjunctivitis: M. Rimas et al., Allergy 45, 18 (1990); in allergic rhinitis: M. Schata et al., J. Allergy Clin. Immunol. 87, 873 (1991). Review of pharmacology and therapeutic use: K. L. Dechant, K. L. Goa, Drugs 41, 202-224 (1991).

Chemical structure

Derivative

Hydrochloride.

Nomenclature

CAS number: 79547-78-7
R-50547; Levophta (Chauvin); Livostin (Novartis).
C26H29FN2O2.HCl; mol wt 456.98.
C 68.34%, H 6.62%, F 4.16%, N 6.13%, O 7.00%, Cl 7.76%.

Therapeutic Category

Antihistaminic.

Keywords

Antihistaminic