Evidence for Possible Involvement of 5-HT _2B Receptors in the Cardiac Valvulopathy Associated With Fenfluramine and Other Serotonergic Medications

Abstract

Our data imply that activation of 5-HT(2B) receptors is necessary to produce VHD and that serotonergic medications that do not activate 5-HT(2B) receptors are unlikely to produce VHD. We suggest that all clinically available medications with serotonergic activity and their active metabolites be screened for agonist activity at 5-HT(2B) receptors and that clinicians should consider suspending their use of medications with significant activity at 5-HT(2B) receptors.

H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs

“…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 H 1 -histamine receptor, which was cloned via PCR amplification of 'Quick-Clone' human cDNA (Clontech) and subcloned via NotI adaptors into the pUNIV-SIG expression vector (Kroeze Roth, unpublished vector sequence). The entire coding region was sequenced by automated dsDNA sequencing (Cleveland Genomics, Cleveland, OH) to verify that PCR-induced mutations had not occurred.…”

“…All binding assays were as previously described (Glennon et al, 2000;Rothman et al, 2000), primarily using cloned human receptor preparations. On-line protocols are available at http://pdsp.cwru.edu.…”

Aripiprazole, A Novel Atypical Antipsychotic Drug with a Unique and Robust Pharmacology

“…A large number of transiently and stably transfected cloned human cDNAs, obtained via the resources of the National Institute of Mental Health Psychoactive Drug Screening Program (NIMH-PDSP), were used for radioligand binding and functional assays as previously detailed (Rothman et al, 2000;Tsai et al, 2000). Conditions for radioligand binding assays, along with K D values for standard compounds, are listed in Table 1.…”

Pharmacologic analysis of non-synonymous coding h5-HT2A SNPs reveals alterations in atypical antipsychotic and agonist efficacies

“…pdsp.cwru.edu). 45 The following mutagenesis primers were obtained from Invitrogen: SNPs were introduced into the cloned human 5-HT 2A receptor template using the QuikChange site directed, PCR-based mutagenesis kit exactly as described by the manufacturer (Stratagene, La Jolla, CA, USA). Mutagenized clones were isolated and subjected to automated DNA sequencing to verify the entire coding sequence for the presence of the desired mutation and the absence of any PCR-induced sequence errors.…”