title: Synthesis, neuropsychopharmacological effects and analgesic-antiinflammatory activities of pyrrole analogues of lefetamine.
abstract: The synthesis of pyrrole analogues of the analgesic drug lefetamine is reported. These derivatives bear the 1-phenyl-2-(1H-pyrrol-1-yl)ethylamino moiety. Compounds were evaluated for analgesic activities in mice by the hot plate and Randall-Selitto tests. Antiinflammatory activity was tested by the carrageenan-induced rat paw edema method. General neuropsychopharmacological effects were also screened. The most interesting compound, N,N-dimethyl-1-phenyl-2-(1H-pyrrol-1-yl)ethylamine, showed an analgesic effect comparable to that of lefetamine, but devoid of the neurotoxicity of this drug.
authors.affiliation: Dipartimento di Studi Farmaceutici, Facoltà di Farmacia, Università degli Studi di Roma La Sapienza, Italy.
authors.forename: S
authors.initials: S
authors.lastname: Massa
authors.forename: G
authors.initials: G
authors.lastname: Stefancich
authors.forename: M
authors.initials: M
authors.lastname: Artico
authors.forename: F
authors.initials: F
authors.lastname: Corelli
authors.forename: R
authors.initials: R
authors.lastname: Silvestri
authors.forename: G C
authors.initials: GC
authors.lastname: Pantaleoni
authors.forename: D
authors.initials: D
authors.lastname: Fanini
authors.forename: G
authors.initials: G
authors.lastname: Palumbo
authors.forename: R
authors.initials: R
authors.lastname: Giorgi
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis*; D000927:Anticonvulsants / Q000138:chemical synthesis; D055598:Chemical Phenomena; D002621:Chemistry; D005106:Exploratory Behavior / Q000187:drug effects; D005260:Female; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009125:Muscle Relaxants, Central / Q000138:chemical synthesis; D010627:Phenethylamines / Q000138:chemical synthesis / Q000494:pharmacology*; D011597:Psychomotor Performance / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D011930:Reaction Time / Q000187:drug effects
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D000927:Anticonvulsants; D009125:Muscle Relaxants, Central; D010627:Phenethylamines; C011896:lephetamine