[Esters of beta-carboline-3-carboxylic acids with alicyclic alcohols--synthesis and benzodiazepine receptor affinity].
Esters of beta-carboline-3-carboxylic acid with alicyclic substituents were prepared and tested with respect to their affinity for the benzodiazepine receptor in mouse brain membranes. Compounds 3d,f and 4b showed high affinities (less than 70 nmol). In the case of 3f the benzodiazepine moiety may be responsible for the affinity. In the GABA-shift test 4b behaves as invers agonists to the benzodiazepine receptor. Further structure-affinity relationships are reported.
Geldsetzer
K H
KH
Institut für Pharmazie, Freien Universität Berlin.
Schunack
W
W
D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology; D001569:Benzodiazepines; D002243:Carbolines / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D004952:Esters / Q000138:chemical synthesis / Q000494:pharmacology; D066298:In Vitro Techniques; D051379:Mice; D011963:Receptors, GABA-A / Q000187:drug effects*
D014151:Anti-Anxiety Agents; D002243:Carbolines; D004952:Esters; D011963:Receptors, GABA-A; D001569:Benzodiazepines
Ester der beta-Carbolin-3-carbonsäure mit alizyklischen Alkoholen-Synthese und Affinität zu Benzodiazepinrezeptoren.