The discovery of new anesthetics by targeting GABA(A) receptors.
Expert Opin Drug Discov
; 6(11): 1187-201, 2011 Nov.
Article
em En
| MEDLINE
| ID: mdl-22646986
ABSTRACT
INTRODUCTION:
Many of the general anesthetics, currently used in clinical practice, work through interactions with GABA(A) receptors. The last 2 decades has witnessed substantial progress in defining the molecular mechanisms by which general anesthetics interact with GABA(A) receptor sites. However, despite progress in the basic scientific understanding of the mechanism of action of general anesthetics, introduction of novel general anesthetic agents into clinical practice has proven quite challenging. AREAS COVERED The focus of this review is on the potential for translating basic science advances into the design of new and improved anesthetics. The authors review general anesthetics in current practice as well as anesthetic drug candidates in development and discuss the potential for novel anesthetic drug development. EXPERT OPINION Opportunities for the discovery of new anesthetics include computational-based ligand-design, structure-based design, re-exploration of old structure-activity data, absorption, distribution, metabolism, excretion and toxicity predictions and high-throughput screening. The authors believe a lack of high-resolution three-dimensional structures of mammalian GABA(A) receptors remains a significant limiting factor in structure-based anesthetic drug design.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Tipo de estudo:
Prognostic_studies
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article