title: [Novel central dopaminergic agents derived from atypical di-substituted 2-aminoindane-4, 7. Synthesis and central pharmacological profile].
abstract: In recent decades, many compounds with central dopaminergic activity have been designed, synthesized and evaluated pharmacologically. However, it has not been possible to obtain a drug able to improve or cure diseases involving dopaminergic regulation in the central nervous system, such as Parkinson's disease and schizophrenia, among others. Taking into consideration the term "atypical pharmacophore" and from the compound 5, the aralkyl fragment was incorporated, and the compounds 10, 11, 13a-h and 14a-h were synthesized. Both the compounds 10 and 13a-h under its methoxylated form and the compounds 11 and 14a-h under the phenolic form, were evaluated to determine their pharmacologically agonistic and antagonistic effects on central dopaminergic activity. For this, the effect of intracerebroventricular injection of said compounds on the hydromineral balance and stereotyped behavior in rats, was determined. The results of the preliminary pharmacological evaluation show a centrally acting action through dopamine mechanisms, in which the compounds 10, 11, 13d-h and 14a showed responses as agonists, whereas compounds 14b-h, had responses as antagonists.
authors: Rosa Elena
authors: RE
authors: Ferrer-Mavárez
authors: Noribel Coromoto
authors: NC
authors: Urdaneta-Gutierrez
authors: Nicole
authors: N
authors: Porta-Knabenschuh
authors: Lucía Chiquinquirá
authors: LC
authors: Rodríguez-Villasmil
authors: Cecire Carolina
authors: CC
authors: Rosales-Peña
authors: Gustavo Adolfo
authors: GA
authors: Espinoza
authors: Ligia Biagina
authors: LB
authors: Angel-Migliore
authors: Katherin del Carmen
authors: Kdel C
authors: Balza-Jiménez
authors: Luis Eduardo
authors: LE
authors: Perdomo-Zavarce
authors: Andrés Rafael
authors: AR
authors: Faría-Quintero
authors: Akram Samear
authors: AS
authors: Dabian-Makarem
authors: Mariana Vanessa
authors: MV
authors: Zapata-Cárdenas
authors: Aarón Raúl
authors: AR
authors: Linero-Arrieta
authors: Gustavo Adolfo
authors: GA
authors: Acurero-Castellano
authors: Anita
authors: A
authors: Israel-Stern
authors: María
authors: M
authors: Rosario Garrido
authors: Heberto
authors: H
authors: Suárez-Roca
authors: Biagina del Carmen
authors: Bdel C
authors: Migliore de Angel
authors: Simón Enrique
authors: SE
authors: Lopez-D'Sola
authors: Jaime
authors: J
authors: Charris-Charris
authors: María Matilde
authors: MM
authors: Ramírez-Moran
authors: Jorge Eduardo
authors: JE
authors: Angel-Guío
mesh_terms: D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D018491:Dopamine Agonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018492:Dopamine Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007189:Indans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007276:Injections, Intraventricular; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D013239:Stereotyped Behavior / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D018491:Dopamine Agonists; D018492:Dopamine Antagonists; D007189:Indans; C006545:2-aminoindan