Peripheral selectivity of the novel cannabinoid receptor antagonist TM38837 in healthy subjects

• Published in: British journal of clinical pharmacology Vol. 76; no. 6; pp. 846 - 857
• Main Authors: Klumpers, Linda E., Fridberg, Marianne, Kam, Marieke L., Little, Paul B., Jensen, Niels Ole, Kleinloog, Hendrik D., Elling, Christian E., Gerven, Joop M. A.
• Format: Journal Article
• Language: English
• Published: England Blackwell Science Inc 01.12.2013
• Subjects: Adolescent; Adult; Blood Pressure - drug effects; Cannabinoid Receptor Agonists - pharmacology; Cannabinoid Receptor Antagonists - administration & dosage; Cannabinoid Receptor Antagonists - adverse effects; Cannabinoid Receptor Antagonists - pharmacokinetics; Cannabinoid Receptor Antagonists - pharmacology; cannabinoid receptor type 1 antagonist; Clinical Trials; Cross-Over Studies; Dose-Response Relationship, Drug; Double-Blind Method; Dronabinol - pharmacology; Healthy Volunteers; Heart Rate - drug effects; Humans; Male; Middle Aged; Models, Biological; peripheral CB1 antagonist; Peripheral Nervous System - drug effects; pharmacokinetics; Piperidines - administration & dosage; Piperidines - adverse effects; Piperidines - pharmacokinetics; Piperidines - pharmacology; PK−PD; Pyrazoles - administration & dosage; Pyrazoles - adverse effects; Pyrazoles - pharmacokinetics; Pyrazoles - pharmacology; Receptor, Cannabinoid, CB1 - agonists; Receptor, Cannabinoid, CB1 - antagonists & inhibitors; rimonabant; TM38837; Young Adult; pharmacokinetics; cannabinoid receptor type 1 antagonist; PK−PD; rimonabant; peripheral CB1 antagonist; TM38837

Aim Cannabinoid receptor type 1 (CB1) antagonists show central side effects, whereas beneficial effects are most likely peripherally mediated. In this study, the peripherally selective CB1 antagonist TM38837 was studied in humans. Methods This was a double‐blind, randomized, placebo‐controlled, cros...