Neurochemical studies with the potential antipsychotic compound trans-5-Chloro-2-methyl-2,3,3a,12b-tetrahydro-1H- dibenz[2,3:6,7]oxepino[4,5-c]pyrrolidine maleate.
trans-5-Chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz [2,3:6,7]oxepino[4,5-c]pyrrolidine maleate (Org 5222) has dopamine D2 antagonistic and negligible anticholinergic properties of the classical neuroleptic haloperidol. In addition it combines the strong antiserotonergic and antihistaminergic properties of chlorpromazine and clozapine with the potent dopamine D-1 antagonistic properties of Sch 23390 (R-(+)-delta-chloro-2,3,4,5-tetrahydro-3-methyl-5- phenyl-1H-3-benazepin-7-ol(Z)-2-buteneoate). This in conjunction to its behavioural properties, warrants clinical testing in psychotic patients.
De Boer
T
T
Scientific Development Group, Organon International B.V., Pharma Division Akzo, Oss, The Netherlands.
Tonnaer
J A
JA
De Vos
C J
CJ
Van Delft
A M
AM
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D000818:Animals; D014150:Antipsychotic Agents / Q000494:pharmacology*; D001058:Apomorphine / Q000031:analogs & derivatives / Q000378:metabolism; D001341:Autonomic Nervous System / Q000187:drug effects; D001552:Benzazepines / Q000378:metabolism; D001923:Brain Chemistry / Q000187:drug effects*; D003342:Corpus Striatum / Q000187:drug effects / Q000378:metabolism; D000242:Cyclic AMP / Q000096:biosynthesis; D003986:Dibenzocycloheptenes; D003990:Dibenzoxepins / Q000494:pharmacology*; D006576:Heterocyclic Compounds, 4 or More Rings; D066298:In Vitro Techniques; D008297:Male; D008566:Membranes / Q000187:drug effects / Q000378:metabolism; D008803:Mianserin / Q000378:metabolism; D011224:Prazosin / Q000378:metabolism; D011813:Quinuclidinyl Benzilate / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D012701:Serotonin / Q000378:metabolism; D013764:Tetrahydronaphthalenes / Q000378:metabolism; D015016:Yohimbine / Q000378:metabolism
D014150:Antipsychotic Agents; D001552:Benzazepines; D003986:Dibenzocycloheptenes; D003990:Dibenzoxepins; D006576:Heterocyclic Compounds, 4 or More Rings; D013764:Tetrahydronaphthalenes; D008803:Mianserin; D015016:Yohimbine; D012701:Serotonin; C009074:N-n-propylnorapomorphine; D011813:Quinuclidinyl Benzilate; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D000242:Cyclic AMP; C522667:asenapine; D001058:Apomorphine; D011224:Prazosin