[Novel central dopaminergic agents derived from atypical di-substituted 2-aminoindane-4, 7. Synthesis and central pharmacological profile].

Journal Article (Journal Article;English 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.

Duke Authors

Cited Authors

  • Ferrer-Mavárez, RE; Urdaneta-Gutierrez, NC; Porta-Knabenschuh, N; Rodríguez-Villasmil, LC; Rosales-Peña, CC; Espinoza, GA; Angel-Migliore, LB; Balza-Jiménez, KDC; Perdomo-Zavarce, LE; Faría-Quintero, AR; Dabian-Makarem, AS; Zapata-Cárdenas, MV; Linero-Arrieta, AR; Acurero-Castellano, GA; Israel-Stern, A; Rosario Garrido, M; Suárez-Roca, H; Migliore de Angel, BDC; Lopez-D'Sola, SE; Charris-Charris, J; Ramírez-Moran, MM; Angel-Guío, JE

Published Date

  • June 2015

Published In

Volume / Issue

  • 56 / 2

Start / End Page

  • 137 - 154

PubMed ID

  • 26299055

International Standard Serial Number (ISSN)

  • 0535-5133

Language

  • spa