Probing the function of 5-HT(1B/1D) receptors in psychiatric patients

Journal article

Pharmacological challenge tests provide a method of assessing the functional responsiveness of serotonin (5-HT) receptor subtypes in the human brain. A number of selective agonist ligands for the 5-HT(1B/1D) receptor are available for human use; however, these compounds do not distinguish between 5-HT(1B) and 5-HT(1D) receptors, which is somewhat of a disadvantage. Acute administration of sumatriptan, rizatriptan, and zolmitriptan all increase plasma growth hormone in healthy subjects, possibly via activation of postsynaptic 5-HT(1D) receptors. This response is blunted in major depression. Sumatriptan lowers plasma prolactin, perhaps via activation of presynaptic 5-HT(1B) receptors. This response is not altered during repeated treatment with selective serotonin reuptake inhibitors (SSRIs), suggesting that 5-HT(1B) receptors retain the ability to restrain 5-HT outflow during short-term SSRI treatment.

Authors: Whale, R; Cowen, P

• Journal: CNS Spectrums
• Volume: 3
• Issue: 8
• Pages: 40-45
• Publication date: 1998-01-01
• ISSN: 1092-8529
• Language: English