ZK-93426 explained

ZK-93426 (ethyl-5-isopropoxy-4-methyl-beta-carboline-3-carboxylate) is a drug from the beta-carboline family. It acts as a weak partial inverse agonist of benzodiazepine receptors,^[1] meaning that it causes the opposite effects to the benzodiazepine class of drugs and has anxiogenic properties,^[2] although unlike most benzodiazepine antagonists it is not a convulsant and actually has weak anticonvulsant effects.^[3] In human tests it produced alertness, restlessness and feelings of apprehension, and reversed the effect of the benzodiazepine lormetazepam.^{[4] [5]} It was also shown to produce nootropic effects^{[6] [7]} and increased release of acetylcholine.^{[8] [9]}

See also

• ZK-93423

References

1. Camerman . A . Mastropaolo . D . Hempel . A . Camerman . N . Ethyl 5-isopropoxy-4-methyl-beta-carboline-3-carboxylate: structural determinants of benzodiazepine-receptor antagonism . Acta Crystallographica C . 61 . Pt 4 . o265–6 . 2005 . 15805647 . 10.1107/S0108270105005457 . 2005AcCrC..61O.265C .
2. File . SE . Pellow . S . Jensen . LH . Actions of the beta-carboline ZK 93426 in an animal test of anxiety and the holeboard: interactions with Ro 15-1788 . Journal of Neural Transmission . 65 . 2 . 103–14 . 1986 . 3009709 . 10.1007/BF01256486 . 7230560 .
3. Jensen . LH . Petersen . EN . Braestrup . C . Honoré . T . Kehr . W . Stephens . DN . Schneider . H . Seidelmann . D . Schmiechen . R . Evaluation of the beta-carboline ZK 93 426 as a benzodiazepine receptor antagonist . Psychopharmacology . 83 . 3 . 249–56 . 1984 . 6089247 . 10.1007/BF00464789 . 37990146 .
4. Dorow . R . Duka . T . Höller . L . Sauerbrey . N . Clinical perspectives of beta-carbolines from first studies in humans . Brain Research Bulletin . 19 . 3 . 319–26 . 1987 . 2890423 . 10.1016/0361-9230(87)90100-6. 54287050 .
5. Duka . T . Goerke . D . Dorow . R . Höller . L . Fichte . K . Human studies on the benzodiazepine receptor antagonist beta-carboline ZK 93 426: antagonism of lormetazepam's psychotropic effects . Psychopharmacology . 95 . 4 . 463–71 . 1988 . 2905500 . 10.1007/bf00172956. 25383323 .
6. Book: Duka . T . Edelmann . V . Schütt . B . Dorow . R . Benzodiazepine Receptor Ligands, Memory and Information Processing . β-Carbolines as Tools in Memory Research: Human Data with the β-Carboline ZK 93426 . Psychopharmacology Series . 6 . 246–60 . 1988 . 3064085 . 10.1007/978-3-642-73288-1_18. 978-3-642-73290-4 .
7. Duka . T . Ott . H . Rohloff . A . Voet . B . The effects of a benzodiazepine receptor antagonist beta-carboline ZK-93426 on scopolamine-induced impairment on attention, memory and psychomotor skills . Psychopharmacology . 123 . 4 . 361–73 . 1996 . 8867876 . 10.1007/BF02246647. 36950692 .
8. Moore . H . Sarter . M . Bruno . JP . Age-dependent modulation of in vivo cortical acetylcholine release by benzodiazepine receptor ligands . Brain Research . 596 . 1–2 . 17–29 . 1992 . 1334777 . 10.1016/0006-8993(92)91527-L. 39356368 .
9. Moore . H . Sarter . M . Bruno . JP . Bidirectional modulation of stimulated cortical acetylcholine release by benzodiazepine receptor ligands . Brain Research . 627 . 2 . 267–74 . 1993 . 8298971 . 10.1016/0006-8993(93)90330-P. 29549067 .