Crestani F Martin JR Möhler H Rudolph U 2000 Zolpidem is a widely used hypnotic agent acting at the GABA(A) receptor benzodiazepine site. On recombinant receptors, zolpidem displays a high affinity to alpha 1-GABA(A) receptors, an intermediate affinity to alpha(2)- and alpha(3)-GABA(A) receptors and fails to bind to alpha(5)-GABA(A) receptors. However, it is not known which receptor subtype is essential for mediating the sedative-hypnotic action in vivo. Studying alpha1(H101R) mice, which possess zolpidem-insensitive alpha(1)-GABA(A) receptors, we show that the sedative action of zolpidem is exclusively mediated by alpha(1)-GABA(A) receptors. Similarly, the activity of zolpidem against pentylenetetrazole-induced tonic convulsions is also completely mediated by alpha(1)-GABA(A) receptors. These results establish that the sedative-hypnotic and anticonvulsant activities of zolpidem are due to its action on alpha(1)-GABA(A) receptors and not on alpha(2)- or alpha(3)-GABA(A) receptors. application/pdf https://sonar.ch/global/documents/161790 eng info:eu-repo/semantics/altIdentifier/doi/10.1038/sj.bjp.0703717 info:eu-repo/semantics/altIdentifier/pmid/11090095 info:eu-repo/semantics/openAccess British journal of pharmacology. - 2000 Animals Anticonvulsants Convulsants Diazepam Dose-Response Relationship, Drug Female GABA Antagonists Hypnotics and Sedatives Male Mice Mice, Inbred Strains Mice, Mutant Strains Motor Activity Pentylenetetrazole Pyridines Receptors, GABA-A Zolpidem Mechanism of action of the hypnotic zolpidem in vivo. http://purl.org/coar/resource_type/c_6501