PYPERAZINE DERIVATIVES OF ALKYL-OXINDOLES

Piperazine derivatives of alkyl oxindoles (I) or their acid addition salts are new. Piperazine derivatives of alkyl oxindoles of formula (I) or their acid addition salts are new. R 1 and R 2H, halo, 1-7C alkyl, 1-7C alkoxy or trifluoromethyl; R 3H; R 4 and R 5linear or branched 1-7C alkyl or alkoxy, or H, halo, or trifluoromethyl; m : 1 - 4. An independent claim is included for the preparation of (I). [Image] ACTIVITY : CNS-Gen.; Antidepressant; Tranquilizer; Neuroleptic; Antimanic; Nootropic; Cerebroprotective; Vasotropic; Neuroprotective; Cardiovascular-Gen.; Hypotensive; Gastrointestinal-Gen. MECHANISM OF ACTION : 5-Hydroxytryptamine (5-HT 7) receptor binder; alpha 1 receptor binder; Sinaptosomal serotonin uptake inhibitor. The efficacy of 3-{4-[4-(3-chlorophenyl)-piperazin-1-yl]-butyl}-1,3-dihydro-2H-indol-2-one (a1) was tested for binding to 5-HT 7 receptor. For determination of 5-HT 7 receptor binding, human cloned receptors were used and 3 ETA -lizergic acid diethyl amide (LSD) (1 nM) and 3 ETA -prazosine (0.3 nM) were used as ligands. The measurements of non-specific binding were performed using clozapine (25 mu M) and prazosine (1 mu M). It was observed that (a1) showed a K i value of less than 100 M/l.