[The 5-HT1A receptor: a new effective principle in psychopharmacologic therapy?]

The 5-hydroxytryptamine (5-HT)1A receptor has been the focus of considerable research effort over a decade. However, the definitive classification of this receptor and the full characterization of its pharmacology is still in progress. On the one hand, the selective serotonin-1A receptor partial agonist anxiolytics were developed first and represented a new class of pharmacological agents that have demonstrated efficacy in the treatment of generalized anxiety disorder (GAD). These compounds (e.g. buspirone, gepirone, tandospirone or ipsapirone) offered a completely different pharmacologic approach to this disorder from previous medications as benzodiazepines or alcohol. On the other hand, beta-adrenoceptor blockers (e.g. [-]-pindolol, [-]-propranolol) have been shown to have antagonistic properties on the 5-HT1A receptor side. Preliminary results suggest that beta-adrenoceptor blockers may be useful as adjunctive medication in the treatment of depression by augmenting the antidepressant efficacy of selective serotonin reuptake inhibitors. As the beta-adrenoceptor blockers show also affinities to other 5-HT receptors than the 5-HT1A receptor the recently discovered more selective 5-HT1A antagonists became of interest. The pharmacological properties and potential therapeutic utility of these novel compounds will also be discussed.