PMID- 10209232
OWN - NLM
STAT- MEDLINE
DCOM- 19990603
LR  - 20191103
VI  - 29
IP  - 2-3
DP  - 1999 Apr
TI  - An update on GABAA receptors.
PG  - 196-217
AB  - Recent advances in molecular biology and complementary information derived from
      neuropharmacology, biochemistry and behavior have dramatically increased our
      understanding of various aspects of GABAA receptors. These studies have revealed 
      that the GABAA receptor is derived from various subunits such as alpha1-alpha6,
      beta1-beta3, gamma1-gamma3, delta, epsilon, pi, and rho1-3. Furthermore, two
      additional subunits (beta4, gamma4) of GABAA receptors in chick brain, and five
      isoforms of the rho-subunit in the retina of white perch (Roccus americana) have 
      been identified. Various techniques such as mutation, gene knockout and
      inhibition of GABAA receptor subunits by antisense oligodeoxynucleotides have
      been used to establish the physiological/pharmacological significance of the
      GABAA receptor subunits and their native receptor assemblies in vivo. Radioligand
      binding to the immunoprecipitated receptors, co-localization studies using
      immunoaffinity chromatography and immunocytochemistry techniques have been
      utilized to establish the composition and pharmacology of native GABAA receptor
      assemblies. Partial agonists of GABAA receptors are being developed as
      anxiolytics which have fewer and less severe side effects as compared to
      conventional benzodiazepines because of their lower efficacy and better
      selectivity for the GABAA receptor subtypes. The subunit requirement of various
      drugs such as anxiolytics, anticonvulsants, general anesthetics, barbiturates,
      ethanol and neurosteroids, which are known to elicit at least some of their
      pharmacological effects via the GABAA receptors, have been investigated during
      the last few years so as to understand their exact mechanism of action.
      Furthermore, the molecular determinants of clinically important drug-targets have
      been investigated. These aspects of GABAA receptors have been discussed in detail
      in this review article.
CI  - Copyright 1999 Elsevier Science B.V.
FAU - Mehta, A K
AU  - Mehta AK
AD  - Department of Pharmacology, The University of Texas Health Science Center at San 
      Antonio, 7703 Floyd Curl Drive, San Antonio, TX 78284-7764, USA.
FAU - Ticku, M K
AU  - Ticku MK
LA  - eng
GR  - AA04090/AA/NIAAA NIH HHS/United States
GR  - NS15339/NS/NINDS NIH HHS/United States
GR  - NS24339/NS/NINDS NIH HHS/United States
GR  - etc.
PT  - Journal Article
PT  - Research Support, U.S. Gov't, P.H.S.
PT  - Review
PL  - Netherlands
TA  - Brain Res Brain Res Rev
JT  - Brain research. Brain research reviews
JID - 8908638
RN  - 0 (GABA-A Receptor Agonists)
RN  - 0 (GABA-A Receptor Antagonists)
RN  - 0 (Receptors, GABA-A)
SB  - IM
MH  - Animals
MH  - GABA-A Receptor Agonists
MH  - GABA-A Receptor Antagonists
MH  - Humans
MH  - Receptors, GABA-A/drug effects/*physiology
RF  - 370
EDAT- 1999/04/21 00:00
MHDA- 1999/04/21 00:01
CRDT- 1999/04/21 00:00
PHST- 1999/04/21 00:00 [pubmed]
PHST- 1999/04/21 00:01 [medline]
PHST- 1999/04/21 00:00 [entrez]
AID - S0165-0173(98)00052-6 [pii]
AID - 10.1016/s0165-0173(98)00052-6 [doi]
PST - ppublish
SO  - Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. doi:
      10.1016/s0165-0173(98)00052-6.