Chemistry and Pharmacology of the 1,4-Benzodiazepines

Parametria da associação do midazolam ou diazepam em cães pré-tratados pela atropina e tratados pela dexmedetomidina e quetamina

“…Os benzodiazepínicos exibem efeitos ansiolíticos, tranquilizantes, hipnóticos, miorrelaxantes e provocam amnésia e alterações psicomotoras (RANDALL et al, 1974), agindo fundamentalmente sobre o sistema límbico reduzindo a atividade funcional do hipotálamo e córtex, com ação do ácido gamaaminobutírico (GABA) como neurotransmissor inibitor do sistema nervoso central (SPINOSA et al, 2002). O diazepam e o midazolam são os dois agentes mais empregados, sendo o midazolam um fármaco de meia vida (1,7 hora) mais curta que a diazepam com maior potência hipnótica (FANTONI & CORTOPASSI, 2002).…”

The binding of [3H]‐diazepam to guinea‐pig ileal longitudinal muscle and the in vitro inhibition of contraction by benzodiazepines

“…Benzodiazepines (Bzds) have long been used for their anxiolytic, anti-convulsant, muscle relaxant and sedative-hypnotic properties (Zbinden & Randall, 1967; Randall, Schallek, Sternbach & Ning, 1974;Denber, 1975), although their mechanism of action remains unclear. A major advance was achieved, however, with the discovery of specific and high affinity Bzd receptors in the brain that appear to mediate at least some of the actions of these compounds (Mohler & Okada, 1977;Macherer, Kochman, Bierschenk & Bremner, 1978).…”

Evidence for rotational isomerism of the fluorophenyl ring in the crystal structure of 5-(2-fluorophenyl)-1,3-dihydro-1,6,8-trimethyl-2H-1,4-benzodiazepin-2-one

“…It has been observed that an electron-withdrawing substituent at C(7)is necessary for good in vivo activity (Sternbach, 1973;Randall, Schallek, Sternbach & Ning, 1974); however, these findings are not paralleled by in vitro binding assays. The title compound, which possesses methyl substituents at C(6) and C(8), but no substituent at C(7), binds moderately well to the benzodiazepine receptor, its affinity being about twice that of chlordiazepoxide* (Braestrup & Squires,19 78).…”