6533b7d6fe1ef96bd1266ece
RESEARCH PRODUCT
Zaleplon displays a selectivity to recombinant GABAA receptors different from zolipdem, zopiclone and benzodiazepines
Hartmut LddensKerstin Dmgensubject
ZopicloneZolpidemReceptor complexBenzodiazepineGABAA receptorChemistrymedicine.drug_classStereochemistryGeneral NeurosciencePharmacologyHypnoticZaleplonmedicineReceptormedicine.drugdescription
A chemically heterogeneous group of compounds acts at the benzodiazepine (BZ) recognition site of the γ-aminobutyric acid type A (GABAA) receptor complex. Whereas most 1,4-BZs recognize all GABAA/BZ receptors with similar affinity, other compounds differentiate between the large number of native GABAA receptors which assemble from the more than 14 known subunits. Here we describe the in vitro binding properties of the BZs lorazepam and Ro 15-4513 plus the three hypnotics zaleplon, zolpidem and zopiclone to eight receptors subtypes. Lorazepam fits well into the general shceme for other 1,4-BZs with respect to its receptor subtype selectivity in spite of its clinically different use. Zaleplon but not zolpidem recognizes α2- and α3-receptors that additionally contain a βj and the γ3-subunit. We conclude that the hypnotic zaleplon displays a novel receptor selectivity different from other BZ receptor ligands in clinical use. Furthermore, our data indicate that the α1βjγ2 receptor subtype may be the main mediator of the hypnotic properties of BZ receptor ligands.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 1999-11-01 | Neuroscience Research Communications |