Publication | Open Access
Imidazo[1,2<i>-a</i>]pyrimidines as Functionally Selective and Orally Bioavailable GABA<sub>A</sub>α2/α3 Binding Site Agonists for the Treatment of Anxiety Disorders
132
Citations
17
References
2005
Year
PsychopharmacologyPharmacotherapyExperimental PharmacologySocial SciencesMolecular PharmacologyPharmacological StudyMinimal SedationFunctionally SelectiveHigh-affinity GabaPsychiatryBiochemistryBehavioral NeuroscienceMechanism Of ActionPharmacological AgentNeuropharmacologyPharmacologyFunctional SelectivityNeuroscienceBiological PsychiatryMedicineAnxiety DisordersDrug Discovery
A series of high-affinity GABA(A) agonists with good oral bioavailability in rat and dog and functional selectivity for the GABA(A)alpha2 and -alpha3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g and the 7-propan-2-olimidazopyrimidine 14k are anxiolytic in both conditioned and unconditioned animal models of anxiety with minimal sedation observed at full BZ binding site occupancy.
| Year | Citations | |
|---|---|---|
Page 1
Page 1