Surinabant, a selective cannabinoid receptor type 1 antagonist, inhibits Δ9-tetrahydrocannabinol-induced central nervous system and heart rate effects in humans

British Journal of Clinical Pharmacology

Volumn 76, Issue 1, 2013, Pages 65-77

  Klumpers, Linda E ^a   Roy, Christine ^b   Ferron, Geraldine ^b   Turpault, Sandrine ^b   Poitiers, Franck ^b   Pinquier, Jean Louis ^b   van Hasselt, Johan G C ^a   Zuurman, Lineke ^a   Erwich, Frank A S ^a   van Gerven, Joop M A ^a  

^a CENTRE FOR HUMAN DRUG RESEARCH   (Netherlands)

^b SANOFI   (France)

Author keywords

CB1 receptor antagonist; Pharmacodynamics; Pharmacokinetics; PK PD modelling; SR147778; Surinabant

Indexed keywords

11 HYDROXYDRONABINOL; CANNABINOID 1 RECEPTOR ANTAGONIST; DRINABANT; DRONABINOL; RIMONABANT; SURINABANT; TARANABANT; TETRAHYDROCANNABINOLIC ACID;

ADULT; ANXIETY; AREA UNDER THE CURVE; ARTICLE; BODY EQUILIBRIUM; CANNABIS SMOKING; CENTRAL NERVOUS SYSTEM FUNCTION; CONTROLLED STUDY; CROSSOVER PROCEDURE; DEPRESSION; DIZZINESS; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG DOSE REGIMEN; DRUG EFFECT; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; EUPHORIA; GASTROINTESTINAL DISEASE; HEADACHE; HEART RATE; HUMAN; HUMAN EXPERIMENT; IC 50; IRRITABILITY; MALE; MAXIMUM PLASMA CONCENTRATION; MENTAL DISEASE; NAUSEA; NEUROLOGIC DISEASE; NORMAL HUMAN; OBESITY; PHARMACODYNAMICS; PRIORITY JOURNAL; PROVOCATION TEST; RANDOMIZED CONTROLLED TRIAL; SIDE EFFECT; SINGLE DRUG DOSE; SOMNOLENCE; SUICIDE; TIME TO MAXIMUM PLASMA CONCENTRATION; TOBACCO DEPENDENCE; XEROSTOMIA;

ADOLESCENT; ADULT; CANNABINOID RECEPTOR AGONISTS; CANNABINOID RECEPTOR ANTAGONISTS; CENTRAL NERVOUS SYSTEM; CROSS-OVER STUDIES; DOSE-RESPONSE RELATIONSHIP, DRUG; DOUBLE-BLIND METHOD; DRONABINOL; HEART RATE; HUMANS; MALE; MODELS, BIOLOGICAL; PIPERIDINES; PYRAZOLES; RECEPTOR, CANNABINOID, CB1; YOUNG ADULT;

EID: 84879483888     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/bcp.12071     Document Type: Article

References (41)

1. Mechoulam R, Gaoni Y. A total synthesis of dl-delta-1-tetrahydrocannabinol, the active constituent of hashish. J Am Chem Soc 1965; 87: 3273-3275.
2. Alexander SP, Mathie A, Peters JA. Guide to Receptors and Channels (GRAC). 3rd edn. Br J Pharmacol 2008; 153: (Suppl. 2): S1-209.
3. Munro S, Thomas KL, Abu-Shaar M. Molecular characterization of a peripheral receptor for cannabinoids. Nature 1993; 365: 61-65.
4. Matsuda LA, Lolait SJ, Brownstein MJ, Young AC, Bonner TI. Structure of a cannabinoid receptor and functional expression of the cloned cDNA. Nature 1990; 346: 561-564.
5. Bermudez-Silva FJ, Viveros MP, McPartland JM, Rodriguez FF. The endocannabinoid system, eating behavior and energy homeostasis: the end or a new beginning? Pharmacol Biochem Behav 2010; 95: 375-382.
6. Ravinet TC, Arnone M, Delgorge C, Gonalons N, Keane P, Maffrand JP, Soubrie P. Anti-obesity effect of SR141716, a CB1 receptor antagonist, in diet-induced obese mice. Am J Physiol Regul Integr Comp Physiol 2003; 284: R345-R353.
7. Van Gaal LF, Rissanen AM, Scheen AJ, Ziegler O, Rossner S. Effects of the cannabinoid-1 receptor blocker rimonabant on weight reduction and cardiovascular risk factors in overweight patients: 1-year experience from the RIO-Europe study. Lancet 2005; 365: 1389-1397.
8. Pertwee RG. Emerging strategies for exploiting cannabinoid receptor agonists as medicines. Br J Pharmacol 2009; 156: 397-411.
9. Rinaldi-Carmona M, Barth F, Heaulme M, Shire D, Calandra B, Congy C, Martinez S, Maruani J, Neliat G, Caput D. SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 1994; 350: 240-244.
10. de Rodriguez FF, Roberts AJ, Bilbao A, Koob GF, Navarro M. Cannabinoid receptor antagonist SR141716A decreases operant ethanol self administration in rats exposed to ethanol-vapor chambers. Zhongguo Yao Li Xue Bao 1999; 20: 1109-1114.
11. Centre for Reviews and Dissemination. Health Information Resources. 3-12-2004. Ref Type: Online Source. 2004.
12. Cohen C, Perrault G, Griebel G, Soubrie P. Nicotine-associated cues maintain nicotine-seeking behavior in rats several weeks after nicotine withdrawal: reversal by the cannabinoid (CB1) receptor antagonist, rimonabant (SR141716). Neuropsychopharmacology 2005; 30: 145-155.
13. Cohen C, Perrault G, Voltz C, Steinberg R, Soubrie P. SR141716, a central cannabinoid (CB(1)) receptor antagonist, blocks the motivational and dopamine-releasing effects of nicotine in rats. Behav Pharmacol 2002; 13: 451-463.
14. Wathion N. Public statement on Acomplia (rimonabant): withdrawal of the marketing authorisation in the European Union. 2009. EMEA/39457/2009. 1-30-2009. Ref Type: Internet Communication.
15. The European Medicines Agency (EMEA). The European Medicines Agency recommends suspension of the marketing authorisation of Acomplia. Doc.Ref.EMEA/CHMP/537777/2008. 10-23-2008. Ref Type: Internet Communication. 2008.
16. The European Medicines Agency (EMEA). Questions and answers on the recommendation to suspend the marketing authorisation of Acomplia (rimonabant). Doc.Ref.EMEA/537153/2008. 10-23-2008. Ref Type: Internet Communication. 2008.
17. Merck & Co., Inc. Merck discontinues development of investigational medicine taranabant for obesity. 10-2-2008. Ref Type: Internet Communication. 2008.
18. Aronne LJ, Tonstad S, Moreno M, Gantz I, Erondu N, Suryawanshi S, Molony C, Sieberts S, Nayee J, Meehan AG, Shapiro D, Heymsfield SB, Kaufman KD, Amatruda JM. A clinical trial assessing the safety and efficacy of taranabant, a CB1R inverse agonist, in obese and overweight patients: a high-dose study. Int J Obes (Lond) 2010; 34: 919-935.
19. Kipnes MS, Hollander P, Fujioka K, Gantz I, Seck T, Erondu N, Shentu Y, Lu K, Suryawanshi S, Chou M, Johnson-Levonas AO, Heymsfield SB, Shapiro D, Kaufman KD, Amatruda JM. A one-year study to assess the safety and efficacy of the CB1R inverse agonist taranabant in overweight and obese patients with type 2 diabetes. Diabetes Obes Metab 2010; 12: 517-531.
20. Proietto J, Rissanen A, Harp JB, Erondu N, Yu Q, Suryawanshi S, Jones ME, Johnson-Levonas AO, Heymsfield SB, Kaufman KD, Amatruda JM. A clinical trial assessing the safety and efficacy of the CB1R inverse agonist taranabant in obese and overweight patients: low-dose study. Int J Obes (Lond) 2010; 34: 1243-1254.
21. Morrison MF, Ceesay P, Gantz I, Kaufman KD, Lines CR. Randomized, controlled, double-blind trial of taranabant for smoking cessation. Psychopharmacology (Berl) 2010; 209: 245-253.
22. Kirilly E, Gonda X, Bagdy G. CB1 receptor antagonists: new discoveries leading to new perspectives. Acta Physiol (Oxf) 2012; 205: 41-60.
23. Cohen AF. Developing drug prototypes: pharmacology replaces safety and tolerability? Nat Rev Drug Discov 2010; 9: 856-865.
24. Tonstad S, Aubin HJ. Efficacy of a dose range of surinabant, a cannabinoid receptor blocker, for smoking cessation: a randomized controlled clinical trial. J Psychopharmacol 2012; 26: 1003-1009.
25. Cahill K, Ussher MH. Cannabinoid type 1 receptor antagonists for smoking cessation. Cochrane Database Syst Rev 2011; (3): CD005353.
26. Zuurman L, Roy C, Schoemaker R, Amatsaleh A, Guimaeres L, Pinquier J, Cohen A, van Gerven J. Inhibition of THC-induced effects on the central nervous system and heart rate by a novel CB1 receptor antagonist AVE1625. J Psychopharmacol 2010; 24: 363-371.
27. Zuurman L, Roy C, Schoemaker RC, Hazekamp A, Den Hartigh J, Bender JC, Verpoorte R, Pinquier JL, Cohen AF, van Gerven JM. Effect of intrapulmonary tetrahydrocannabinol administration in humans. J Psychopharmacol 2008; 22: 707-716.
28. Sanofi-aventis. A clinical study to investigate the tolerability and pharmacokinetic parameters of SR147778 after repeated oral administrations (soft gelatin capsules) in young healthy male subjects; CSRCO-TDR5736-EN-E01 - Data on file. 2006. Ref Type: Unpublished Work.
29. Sanofi-Aventis. Excretion balance, pharmacokinetics, metabolites profiling and identification after single oral administration of SR147778 using [14C]-labeled compound in healthy male subjects. Open, non-randomized and single center study, CSRCO-BEX4499-EN-E01 - Data on file. 2006. Ref Type: Unpublished Work.
30. Sanofi-Aventis. Determination of the cytochrome P450 (CYP) isoforms involved in the oxidative metabolism of SR147778 in vitro, CMPKCO-MIH0135-EN-E01 - Data on file. 2006. Ref Type: Unpublished Work.
31. Strougo A, Zuurman L, Roy C, Pinquier JL, van Gerven JM, Cohen AF, Schoemaker RC. Modelling of the concentration-effect relationship of THC on central nervous system parameters and heart rate - insight into its mechanisms of action and a tool for clinical research and development of cannabinoids. J Psychopharmacol 2008; 22: 717-726.
32. Zuurman L, Ippel AE, Moin E, van Gerven JM. Biomarkers for the effects of cannabis and THC in healthy volunteers. Br J Clin Pharmacol 2009; 67: 5-21.
33. Bond A, Lader M. The use of analogue scales in rating subjective feelings. Br J Med Psychol 1974; 47: 211-218.
34. Bowdle TA, Radant AD, Cowley DS, Kharasch ED, Strassman RJ, Roy-Byrne PP. Psychedelic effects of ketamine in healthy volunteers: relationship to steady-state plasma concentrations. Anesthesiology 1998; 88: 82-88.
35. NONMEM project group. NONMEM users guide. 1992. Ref Type: Computer Program.
36. Speth H. A Linux cluster for population pharmacokinetic analyses. Int J Clin Pharmacol Ther 2004; 42: 189-190.
37. Ferron G, Klumpers LE, van Gerven JMA, Roy C. PK and PK/PD modeling of CB1 blocker antagonism of THC induced CNS and heart rate effect. PAGE, Abstracts 17. 2008. Ref Type: Abstract.
38. Huestis MA, Gorelick DA, Heishman SJ, Preston KL, Nelson RA, Moolchan ET, Frank RA. Blockade of effects of smoked marijuana by the CB1-selective cannabinoid receptor antagonist SR141716. Arch Gen Psychiatry 2001; 58: 322-328.
39. Huestis MA, Boyd SJ, Heishman SJ, Preston KL, Bonnet D, Le FG, Gorelick DA. Single and multiple doses of rimonabant antagonize acute effects of smoked cannabis in male cannabis users. Psychopharmacology (Berl) 2007; 194: 505-515.
40. Gomez R, Navarro M, Ferrer B, Trigo JM, Bilbao A, Del AI, Cippitelli A, Nava F, Piomelli D, de Rodriguez FF. A peripheral mechanism for CB1 cannabinoid receptor-dependent modulation of feeding. J Neurosci 2002; 22: 9612-9617.
41. Mager DE, Wyska E, Jusko WJ. Diversity of mechanism-based pharmacodynamic models. Drug Metab Dispos 2003; 31: 510-518.