| 摘要 |
<p>1-amino-1-pyridylaminoalkyl-cyclopropane derivatives (I) are new. 1-amino-1-pyridylaminoalkyl-cyclopropane derivatives of formula (I) are new n : 1-6; R 1, R 2 and R 7hydrogen, 1-6C linear or branched alkyl or arylalkyl; R 3 and R 4hydrogen or 1-6C linear or branched alkyl; R 5 and R 6hydrogen, 1-6C alkyl or alkoxy, halo, hydroxy, cyano, nitro, 2-6C linear or branched acyl, 1-6C alkoxycarbonyl, trihaloalkyl or trihaloalkoxy (all linear or branched), or amino, optionally substituted by 1 or 2 1-6C linear or branched alkyl; aryl : (bi)phenyl, naphthyl (optionally di- or tetra-hydro), indanyl or indenyl, each optionally substituted by one or more of halo, 1-6C alkyl or alkoxy, hydroxy, cyano, nitro, 2-7C acyl, 1-6C alkoxycarbonyl, trihaloalkyl or trihaloalkoxy, or amino, optionally substituted by 1 or 2 1-6C alkyl An independent claim is included for several methods for preparing (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Neuroleptic; Antismoking; Analgesic; Antiparkinsonian. In the social recognition test in rats ( Psychopharmacology, 91 (1987) 363), unspecified (I) were active at 1-3 mg/kg, intraperitoneally, indicating a strong memory-improving effect. MECHANISM OF ACTION : (I) are specific ligands for the central alpha 4beta 2 nicotinic receptors. When tested by the method of Mol. Pharmacol., 39 (1990) 9 for displacement of tritiated cytisine from such receptors in rat brain, unspecified (I) had Ki about 1 nM.</p> |
