GABA(A) and GABA(B) receptor agonists, partial agonists, antagonists and modulators: Design and therapeutic prospects
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GABA(A) and GABA(B) receptor agonists, partial agonists, antagonists and modulators : Design and therapeutic prospects. / Krogsgaard-Larsen, Povl; Frølund, Bente; Kristiansen, Uffe; Frydenvang, Karla; Ebert, Bjarke.
In: European Journal of Pharmaceutical Sciences, Vol. 5, No. 6, 11.1997, p. 355-384.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - GABA(A) and GABA(B) receptor agonists, partial agonists, antagonists and modulators
T2 - Design and therapeutic prospects
AU - Krogsgaard-Larsen, Povl
AU - Frølund, Bente
AU - Kristiansen, Uffe
AU - Frydenvang, Karla
AU - Ebert, Bjarke
N1 - Funding Information: This work was supported by grants from the Danish Technical Research Council, the Lundbeck Foundation, the Alfred Benzon Foundation and the Danish State Biotechnology Programme (1991-1995). The secretarial assistance of Mrs. Anne Nord-ly is gratefully acknowledged.
PY - 1997/11
Y1 - 1997/11
N2 - A large number of highly selective GABA(A) and, more recently, GABA(B) receptor ligands have been developed and used for receptor characterization. Whereas full agonists and antagonists at GABA(A) receptors, for different reasons, may be difficult to use therapeutically, partial GABA(A) agonists may have therapeutic interest. The efficacious partial GABA(A) agonist, THIP, shows analgesic and anxiolytic effects in man, but THIP is ineffective as an antiepileptic agent, and PET studies have disclosed that THIP increases glucose metabolism in epileptic patients and human volunteers. In principle, GABA(A) antagonists may be used therapeutically in Alzheimer's disease and schizophrenia, but low-efficacy partial GABA(A) agonists may have particular interest in these disorders. Using the nonannulated THIP analogue, 4-PIOL, as a lead, a series of partial GABA(A) agonists showing a broad spectrum of relative efficacies have been developed.
AB - A large number of highly selective GABA(A) and, more recently, GABA(B) receptor ligands have been developed and used for receptor characterization. Whereas full agonists and antagonists at GABA(A) receptors, for different reasons, may be difficult to use therapeutically, partial GABA(A) agonists may have therapeutic interest. The efficacious partial GABA(A) agonist, THIP, shows analgesic and anxiolytic effects in man, but THIP is ineffective as an antiepileptic agent, and PET studies have disclosed that THIP increases glucose metabolism in epileptic patients and human volunteers. In principle, GABA(A) antagonists may be used therapeutically in Alzheimer's disease and schizophrenia, but low-efficacy partial GABA(A) agonists may have particular interest in these disorders. Using the nonannulated THIP analogue, 4-PIOL, as a lead, a series of partial GABA(A) agonists showing a broad spectrum of relative efficacies have been developed.
KW - Benzodiazepines
KW - GABA analgesia
KW - GABA(A) agonists
KW - GABA(A) antagonists
KW - GABA(A) partial agonists
KW - GABA(A) receptors
KW - GABA(B) agonists
KW - GABA(B) antagonists
KW - GABA(B) receptors
KW - Neuroactive steroids
KW - Neurosteroids
UR - http://www.scopus.com/inward/record.url?scp=0031282607&partnerID=8YFLogxK
U2 - 10.1016/S0928-0987(97)10009-4
DO - 10.1016/S0928-0987(97)10009-4
M3 - Journal article
AN - SCOPUS:0031282607
VL - 5
SP - 355
EP - 384
JO - Norvegica Pharmaceutica Acta
JF - Norvegica Pharmaceutica Acta
SN - 0928-0987
IS - 6
ER -
ID: 312698989