Evidence for Possible Involvement of 5-HT2B Receptors in the Cardiac Valvulopathy Associated With Fenfluramine and Other Serotonergic Medications

By R. Rothman, M. Baumann, J. Savage, Laura Rauser, A. McBride, S. Hufeisen, Bryan L. Roth. Circulation, 2000

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H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs (2003, positive): “Cloned receptor preparations were obtained via the resources of the NIMH-PDSP as previously detailed (Rothman et al, 2000), with the exception of the human H1-histamine receptor, which was cloned via PCR amplification of ‘Quick-Clone’ human cDNA (Clontech) and subcloned via NotI adaptors into the…”
Aripiprazole, A Novel Atypical Antipsychotic Drug with a Unique and Robust Pharmacology (2003, methodology): “Since agonism at 5-HT2B receptors is associated with vavlular heart disease (Fitzgerald et al, 2000; Rothman et al, 2000), it is important to determine whether aripiprazole was an agonist or antagonist at 5-HT2B receptors.”
In silico pharmacology for drug discovery: applications to targets and beyond (2007, background): “The primary metabolite, norfenfluramine, potently stimulates 5-HT2B (Fitzgerald et al., 2000; Rothman et al., 2000).”
The Expanded Biology of Serotonin (2009, positive): “Serotonin also plays a pathological role in the cardiac valvulopathy caused by the appetite suppressant fenfluramine (see sidebar, Serotonergic Drugs andValvular Heart Disease) (7, 34).”