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Titolo:
GABA(A) AND GABA(B) RECEPTOR AGONISTS, PARTIAL AGONISTS, ANTAGONISTS AND MODULATORS - DESIGN AND THERAPEUTIC PROSPECTS
Autore:
KROGSGAARDLARSEN P; FROLUND B; KRISTIANSEN U; FRYDENVANG K; EBERT B;
Indirizzi:
ROYAL DANISH SCH PHARM,PHARMABIOTEC RES CTR,DEPT MED CHEM DK-2100 COPENHAGEN DENMARK ROYAL DANISH SCH PHARM,PHARMABIOTEC RES CTR,DEPT BIOL DK-2100 COPENHAGEN DENMARK
Titolo Testata:
European journal of pharmaceutical sciences
fascicolo: 6, volume: 5, anno: 1997,
pagine: 355 - 384
SICI:
0928-0987(1997)5:6<355:GAGRAP>2.0.ZU;2-D
Fonte:
ISI
Lingua:
ENG
Soggetto:
CEREBELLAR GRANULE CELLS; AMINOBUTYRIC-ACID RECEPTORS; CENTRAL-NERVOUS-SYSTEM; SENSITIVE CALCIUM CHANNELS; H-3 FLUNITRAZEPAM BINDING; BRAIN GLUCOSE-METABOLISM; EMISSION TOMOGRAPHY PET; RETINAL BIPOLAR CELLS; EPILEPSY TLE PATIENTS; PIG ISOLATED ILEUM;
Keywords:
GABA(A) RECEPTORS; GABA(A) AGONISTS; GABA(A) PARTIAL AGONISTS; GABA(A) ANTAGONISTS; BENZODIAZEPINES; NEUROSTEROIDS; NEUROACTIVE STEROIDS; GABA ANALGESIA; GABA(B) RECEPTORS; GABA(B) AGONISTS; GABA(B) ANTAGONISTS;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
202
Recensione:
Indirizzi per estratti:
Citazione:
P. Krogsgaardlarsen et al., "GABA(A) AND GABA(B) RECEPTOR AGONISTS, PARTIAL AGONISTS, ANTAGONISTS AND MODULATORS - DESIGN AND THERAPEUTIC PROSPECTS", European journal of pharmaceutical sciences, 5(6), 1997, pp. 355-384

Abstract

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, partialGABA(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.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 15:44:47