Trial reportBritish journal of clinical pharmacology2013
Surinabant, a selective cannabinoid receptor type 1 antagonist, inhibits Δ9-tetrahydrocannabinol-induced central nervous system and heart rate effects in humans.
Trial report in British journal of clinical pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
19 citing papers in PubMed.
- CBClinical pharmacology and therapeutics · 2025Trial
- Derivation of a health-based guidance value for ΔEFSA journal. European Food Safety Authority · 2025Article
- The resurgence of synthetic cannabinoid receptor agonists as adulterants in the Era of Cannabis legalization: Lessons from prior epidemics and clinical implications.Neuroscience and biobehavioral reviews · 2025Review
- Review
- Role of Cannabinoid Signaling in Cardiovascular Function and Ischemic Injury.The Journal of pharmacology and experimental therapeutics · 2023Review
- Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies.RSC medicinal chemistry · 2022Review
- Why Do Marijuana and Synthetic Cannabimimetics Induce Acute Myocardial Infarction in Healthy Young People?Cells · 2022Review
- Cannabis and Athletic Performance.Sports medicine (Auckland, N.Z.) · 2021Review
- Therapeutic potential and safety considerations for the clinical use of synthetic cannabinoids.Pharmacology, biochemistry, and behavior · 2020Review
- CannabinoidJournal of neural transmission (Vienna, Austria : 1996) · 2020Review
- Cannabidiol and the Remainder of the Plant Extract Modulate the Effects of Δ9-Tetrahydrocannabinol on Fear Memory Reconsolidation.Frontiers in behavioral neuroscience · 2019Article
- Cardiovascular effects of marijuana and synthetic cannabinoids: the good, the bad, and the ugly.Nature reviews. Cardiology · 2018Review
- A Systematic Review and Meta-Analysis of the In Vivo Haemodynamic Effects of Δ⁸-Tetrahydrocannabinol.Pharmaceuticals (Basel, Switzerland) · 2018Review
- Psychosocial and pharmacological interventions for the treatment of cannabis use disorder.F1000Research · 2018Review
- Pharmacokinetic/pharmaco-dynamic modelling and simulation of the effects of different cannabinoid receptor type 1 antagonists on Δ(9)-tetrahydrocannabinol challenge tests.British journal of clinical pharmacology · 2016Article
- Population pharmacokinetic model of THC integrates oral, intravenous, and pulmonary dosing and characterizes short- and long-term pharmacokinetics.Clinical pharmacokinetics · 2015Article
- Profiling the subjective effects of Δ⁹-tetrahydrocannabinol using visual analogue scales.International journal of methods in psychiatric research · 2014Article
- Modulating the endocannabinoid system in human health and disease--successes and failures.The FEBS journal · 2013Review
- Lessons Learned and Potentials for Improvement in CNS Drug Development: ISCTM Section on Designing the Right Series of Experiments.Innovations in clinical neuroscienceArticle
Corrections and comments
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Authors and funding
10 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimCannabinoid receptor type 1 (CB1 ) antagonists have been developed for the treatment of obesity and associated risk factors. Surinabant is a high affinity CB1 antagonist in vitro. The aim of this study was to assess the magnitude of inhibition by surinabant of CNS effects and heart rate induced by Δ(9) -tetrahydrocannabinol (THC) in humans.
methodsThis was a double-blind, placebo-controlled, randomized, four period six sequence crossover study. Thirty healthy young male occasional cannabis users (<1 per week) were included. A single oral dose of surinabant (5, 20 or 60 mg) or placebo was administered followed 1.5 h later by four intrapulmonary THC doses (2, 4, 6 and 6 mg) or vehicle, administered at 1 h intervals. The wash-out period was 14-21 days. Subjective and objective pharmacodynamic (PD) measurements were performed. A population PK-PD model for THC and surinabant quantified PK and PD effects.
resultsSurinabant 20 and 60 mg inhibited all THC-induced PD effects in a similar range for both doses with inhibition ratios ranging from 68.3% (95% CI = 32.5, 104.2; heart rate) to 91.1% (95% CI = 30.3, 151.8; body sway). IC50 ranged from 22.0 ng ml(-1) [relative standard error (RSE) = 45.2%; body sway] to 58.8 ng ml(-1) (RSE = 44.2%; internal perception). Surinabant 5 mg demonstrated no significant effects.
conclusionsThe dose-related inhibition by surinabant, without any effect of its own, suggests that this compound behaves as a CB1 receptor antagonist in humans at these concentrations. A single surinabant dose between 5 to 20 mg and above was able to antagonize THC-induced effects in humans.
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