TY - JOUR
T1 - GABAA receptor subtypes
T2 - Dissecting their pharmacological functions
AU - Rudolph, Uwe
AU - Crestani, Florence
AU - Möhler, Hanns
PY - 2001/4/1
Y1 - 2001/4/1
N2 - The enhancement of GABA-mediated synaptic transmission underlies the pharmacotherapy of various neurological and psychiatric disorders. GABAA receptors are pluripotent drug targets that display an extraordinary structural heterogeneity: they are assembled from a repertoire of at least 18 subunits (α1-6, β1-3, γ1-3, δ, ε, θ, ρ1-3). However, differentiating defined GABAA receptor subtypes on the basis of function has had to await recent progress in the genetic dissection of receptor subtypes in vivo. Evidence that the various actions of allosteric modulators of GABAA receptors, in particular the benzodiazepines, can be attributed to specific GABAA receptor subtypes will be discussed. Such discoveries could open up new avenues for drug development.
AB - The enhancement of GABA-mediated synaptic transmission underlies the pharmacotherapy of various neurological and psychiatric disorders. GABAA receptors are pluripotent drug targets that display an extraordinary structural heterogeneity: they are assembled from a repertoire of at least 18 subunits (α1-6, β1-3, γ1-3, δ, ε, θ, ρ1-3). However, differentiating defined GABAA receptor subtypes on the basis of function has had to await recent progress in the genetic dissection of receptor subtypes in vivo. Evidence that the various actions of allosteric modulators of GABAA receptors, in particular the benzodiazepines, can be attributed to specific GABAA receptor subtypes will be discussed. Such discoveries could open up new avenues for drug development.
UR - http://www.scopus.com/inward/record.url?scp=0035313382&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0035313382&partnerID=8YFLogxK
U2 - 10.1016/S0165-6147(00)01646-1
DO - 10.1016/S0165-6147(00)01646-1
M3 - Review article
C2 - 11282419
AN - SCOPUS:0035313382
SN - 0165-6147
VL - 22
SP - 188
EP - 194
JO - Trends in Pharmacological Sciences
JF - Trends in Pharmacological Sciences
IS - 4
ER -