Psychopharmacology of 5-HT(1A) receptors.

Journal article

Serotonin(1A) (5-HT(1A)) receptors are located on both 5-HT cell bodies where they act as inhibitory autoreceptors and at postsynaptic sites where they mediate the effects of 5-HT released from nerve terminals. The sensitivity of 5-HT(1A) receptors in humans can be measured using the technique of pharmacological challenge. For example, acute administration of a selective 5-HT(1A) receptor agonist, such as ipsapirone, decreases body temperature and increases plasma cortisol through activation of pre- and postsynaptic 5-HT(1A) receptors, respectively. Use of this technique has demonstrated that unmedicated patients with major depression have decreased sensitivity of both pre- and postsynaptic 5-HT(1A) receptors. Treatment with selective serotonin reuptake inhibitors further down-regulates 5-HT(1A) receptor activity. Due to the hypotheses linking decreased sensitivity of 5-HT(1A) autoreceptors with the onset of antidepressant activity, there is current interest in the therapeutic efficacy of combined treatment with selective serotonin reuptake inhibitors and 5-HT(1A) receptor antagonists.

Authors: Cowen, P

• Publication status: Published
• Journal: Nuclear medicine and biology
• Volume: 27
• Issue: 5
• Pages: 437-439
• Publication date: 2000-07-01
• DOI: 10.1016/s0969-8051(00)00108-6
• EISSN: 1872-9614
• ISSN: 0969-8051
• Language: English
• Keywords: Animals; Receptors, Serotonin; Depression; Serotonin Uptake Inhibitors; Humans; Receptors, Serotonin, 5-HT1