title: [Pharmacokinetic and analgesic properties of tabletized dosage form of RU-1205-new imidazobenzimidazole derivative with kappa agonist activity].
abstract: The pharmacokinetic properties of a new imidazobenzimidazole derivative, compound RU-1205, were studied after peroral administration to rabbits at a dose of 50 mg/kg as a parent substance and in coated tablet dosage form. It was found that RU-1205 tablets are characterized by high values of the relative bioavailability (105.3 +/- 11.7%). The results of hot-plate and vinegar-cramp tests showed that both the dosage form and parent substance produced the same analgesic effect. Granulated RU-1205 produced maximum analgesic effect (138.8% relative to control) within 4-h investigation and retained higher analgesic activity compared to that of parent substance (on the average by 58%, p < 0.05) up to 12 h.
authors.forename: A A
authors.initials: AA
authors.lastname: Spasov
authors.forename: L A
authors.initials: LA
authors.lastname: Smirnova
authors.forename: O Iu
authors.initials: OIu
authors.lastname: Grechko
authors.forename: A I
authors.initials: AI
authors.lastname: Rashchenko
authors.forename: D M
authors.initials: DM
authors.lastname: Shtareva
authors.forename: V A
authors.initials: VA
authors.lastname: Anisimova
mesh_terms: D018712:Analgesics, Non-Narcotic / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D000818:Animals; D001562:Benzimidazoles / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D001682:Biological Availability; D004305:Dose-Response Relationship, Drug; D008297:Male; D009025:Morpholines / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D011817:Rabbits; D013607:Tablets
chemical_list: C586860:9-(2-morpholinoethyl)-2-(4-fluorophenyl)imidazo(1,2-alpha)benzimidazole; D018712:Analgesics, Non-Narcotic; D001562:Benzimidazoles; D009025:Morpholines; D013607:Tablets