The human serotonin 5‐HT2B receptor: Pharmacological link between 5‐HT2 and 5‐HT1D receptors

TLDR

The study aims to characterize the human 5‑HT2B receptor’s pharmacology to inform therapeutic drug development. The human 5‑HT2B receptor was cloned from a liver cDNA library and expressed in COS‑1 cells. The receptor displays species‑specific pharmacology, correlating strongly with rat 5‑HT2B and mouse 5‑HT2B/human 5‑HT1D agonists, and is expressed in liver, kidney, lung, and heart, indicating a role in peripheral 5‑HT1D/5‑HT2‑like cardiovascular functions.

Abstract

The human serotonin 5‐HT2B receptor, isolated from a human liver cDNA library, was transfected in COS‐1 cells. Its pharmacological profile shows divergence with serotonin 5‐HT2B receptors of other species. In particular, although strong correlation is observed between the human and the rat 5‐HT2B receptor pharmacology, the correlation is almost as significant for the mouse 5‐HT2B and the human 5‐HT1D receptor agonists. The major sites of expression of its mRNA are in the human liver and kidney, with detectable expression in lung and heart. Therefore, this human 5‐HT2B receptor could account for functions attributed to the peripheral 5‐HT1D/5‐HT2‐like receptors, especially in the cardiovascular system. Thus, its detailed original pharmacology is of prime importance for therapeutic drug development.