{"schemaVersion":"cwiki-fiche-1.0","identifiers":{"inchiKey":"BNLYOVHLLDBOFZ-LJQANCHMSA-N","prefName":"Selonabant (ANEB-001)","symbol":"Sélonabant","iupacName":"N-tert-butyl-3-[(R)-(4-chlorophenyl)-[2-(trifluoromethyl)phenyl]methoxy]azetidine-1-carboxamide","aliases":["ANEB-001","ANEB 001","Selonabant","V-24343"],"cas":"791848-71-0","pubchemCid":"68902536","chebiId":null,"smiles":"CC(C)(C)NC(=O)N1CC(O[C@H](c2ccc(Cl)cc2)c2ccccc2C(F)(F)F)C1","molecularFormula":"C22H24ClF3N2O2","molecularWeight":440.147840348,"xrefs":{"pubchem":"https://pubchem.ncbi.nlm.nih.gov/compound/68902536"}},"classification":{"family":"ecs_tool","familyLabel":"ECS modulator (research)","origin":"synthetic","originLabel":"Synthétique","structuralClassFr":"Carboxamide d'azétidine, chémotype d'antagoniste du CB1 postérieur à la série des pyrazoles. Le cycle azétidine à quatre chaînons est relié par un pont éther à un carbone benzylique de configuration définie qui porte deux aryles distincts, un chlorophényle et un trifluorométhylphényle, tandis que l'azote du cycle supporte un carboxamide tert-butylé. Cette architecture le rapproche du drinabant, également construit sur une azétidine, et l'éloigne du rimonabant."},"originSynthesis":{"heading":"Origin (research tool)","summaryFr":"An entirely chemical route, described here by class only. The molecule is an azetidine carboxamide: a four-membered azetidine ring bears on its nitrogen a carboxamide function capped by a tert-butyl group, and on one of its carbons an ether bridge linked to a benzylic carbon of defined configuration bearing a chlorophenyl and a trifluoromethylphenyl. That skeleton clearly separates it from the pyrazoles of the first generation of antagonists.","originNote":"A wholly synthetic compound with no natural occurrence. It is in clinical development and is not commercialised.","discovered":"Antagoniste du récepteur CB1 repris par la société américaine Anebulo Pharmaceuticals sous le code ANEB-001, avec une indication entièrement différente de celle qui avait fait échouer ses prédécesseurs : non plus le traitement chronique de l'obésité, mais le traitement d'urgence de l'intoxication aiguë aux cannabinoïdes. Son essai de phase 2 chez le volontaire sain a été publié en 2025 par Gorbenko et collaborateurs, au Centre de recherche sur le médicament humain de Leyde."},"pharmacology":{"summaryFr":"Selonabant reverses the logic that had caused the failure of CB1 receptor antagonists. Rimonabant and its successors were to be taken every day, for months, by people otherwise in good health, in order to lose weight: in that context the adverse psychiatric effects linked to prolonged CB1 blockade proved unacceptable and carried away the entire class after 2008. Selonabant, by contrast, targets a single administration, in an emergency situation, in a person already intoxicated. The balance between benefit and risk is not at all the same, and the need is real: emergency department visits for acute cannabinoid intoxication are rising everywhere cannabis policy has been liberalised, with anxiety, panic attacks, tachycardia and sometimes psychotic episodes, without any specific therapy existing. The phase 2 trial published by Gorbenko and colleagues in 2025 gives the compound with oral Δ9-THC in healthy volunteers and measures what remains of it. The sensation of feeling high falls by up to about 83 per cent at 30 milligrams, self-reported alertness rises again, objectively measured postural instability falls by about a third. Heart rate is not significantly modified. The point of note for what follows is that the 10 milligram dose suffices and is better tolerated, nausea and vomiting becoming more frequent at high doses. The authors conclude that these results justify pursuing development towards the emergency management of acute intoxication.","receptorSummaryFr":"An antagonist of the CB1 receptor, used to occupy the receptor and displace Δ9-THC from it. The phase 2 trial conducted by Gorbenko and colleagues gives the compound together with oral Δ9-THC in healthy volunteers and measures the effect on the manifestations of intoxication. The result is clear: the sensation of feeling high, assessed by visual analogue scale, is reduced by up to about 83 per cent at the 30 milligram dose, self-reported alertness increases, and objectively measured postural instability falls by up to about 31 per cent. The effect on heart rate does not reach statistical significance. The authors note that the 10 milligram dose is both efficacious and well tolerated, nausea and vomiting becoming more frequent at high doses.","binding":[{"target":"CB1","efficacy":"antagonist","relativeActivity":88,"reported":"Antagonisme central démontré chez l'humain : sensation d'être défoncé réduite jusqu'à 83 pour cent à 30 mg (Gorbenko et coll. 2025)","confidence":"medium"},{"target":"CB2","efficacy":"modulator","relativeActivity":8,"reported":"Sélectivité CB1 revendiquée ; valeur non détaillée dans les sources retenues","confidence":"medium"}],"references":[{"label":"Gorbenko et coll. 2025 : le sélonabant, antagoniste du récepteur CB1, bloque les effets aigus du THC chez le volontaire sain, essai randomisé contrôlé de phase 2","pmid":"39898464","doi":null,"url":"https://pubmed.ncbi.nlm.nih.gov/39898464/"}]},"pharmacokinetics":"Le composé est actif par voie orale chez l'humain : dans l'essai de phase 2, il est administré conjointement au Δ9-THC oral et produit un effet mesurable sur les manifestations d'intoxication, ce qui établit une absorption et une pénétration cérébrale suffisantes dans le délai de l'expérience. Les doses étudiées vont de 10 à 100 milligrammes. Les paramètres cinétiques détaillés ne sont pas repris ici.","metabolism":"Aucune description publique détaillée des voies de métabolisation n'est reprise dans la source retenue ici. Le pont éther benzylique, le motif trifluorométhylé et le carboxamide tert-butylé sont des motifs habituellement pris en charge par les oxydations des cytochromes P450, mais il s'agit d'une attente de classe et non d'un résultat mesuré.","detection":"La molécule ne figure pas dans les panels de dépistage courants et n'a pas d'intérêt médicolégal établi. Son dosage plasmatique en contexte clinique relève des méthodes de chromatographie liquide couplée à la spectrométrie de masse en tandem.","subjectiveEffects":{"profile":[{"key":"calm","label":"Calm","description":"Relaxation of body and mind; reduced mental noise without marked drowsiness.","intensity":15},{"key":"focus","label":"Clarity","description":"Sustained attention and clear thinking; functional lucidity, not euphoria.","intensity":35},{"key":"sleep","label":"Sleep","description":"Sedative effect: aids sleep onset and the continuity of deep sleep.","intensity":10},{"key":"appetite","label":"Appetite","description":"Stimulation of hunger and of taste appreciation (the “munchies” effect).","intensity":8},{"key":"uplift","label":"High","description":"Euphoria and sensory intensity; altered perception of time and space.","intensity":8}],"doseRanges":null,"humanDataCharacterised":true},"indications":{"approvedMedicines":[]},"harmProfile":{"unstudiedBanner":false,"bannerTextFr":null,"toxicologyFr":"Les données humaines existent, ce qui distingue ce composé de la plupart des molécules de cette famille. Gorbenko et collaborateurs rapportent une tolérance globalement satisfaisante, sans modification cliniquement significative de l'humeur, et une fréquence accrue de nausées et de vomissements aux doses élevées, la dose de 10 milligrammes étant à la fois efficace et bien tolérée. Ce profil doit se lire avec l'antécédent de la classe : les effets psychiatriques indésirables qui ont conduit au retrait du rimonabant sont apparus sous administration chronique, situation différente de l'administration unique en urgence visée ici."},"legal":{"scheduleStatus":"unscheduled","scheduleLabel":"Unscheduled","frScheduleStatus":"unscheduled","tiers":[{"jurisdiction":"international","jurisdictionLabel":"International","label":"Non inscrit aux conventions de contrôle","reference":null,"url":null,"effectiveDate":null,"lastVerified":"2026-05-01","supersededBy":null},{"jurisdiction":"eu","jurisdictionLabel":"Union européenne","label":"Non autorisé ; en développement clinique","reference":null,"url":null,"effectiveDate":null,"lastVerified":"2026-05-01","supersededBy":null},{"jurisdiction":"fr","jurisdictionLabel":"France","label":"Non inscrit ; sans autorisation de mise sur le marché","reference":null,"url":null,"effectiveDate":null,"lastVerified":"2026-05-01","supersededBy":null}],"sourcesFr":"EUR-Lex, UNODC, CND, ANSM, IUPHAR/BPS, ChEBI, EUDA."},"references":[{"label":"Gorbenko et coll. 2025 : le sélonabant, antagoniste du récepteur CB1, bloque les effets aigus du THC chez le volontaire sain, essai randomisé contrôlé de phase 2","pmid":"39898464","doi":null,"url":"https://pubmed.ncbi.nlm.nih.gov/39898464/"}],"meta":{"slug":"selonabant","url":"https://en.phytogrammes.com/wiki/selonabant","lastVerified":"2026-05-01","dataUpdatedAt":"2026-08-17","confidence":"medium","dataCompletenessPct":90,"disclaimerFr":"Contenu éditorial informatif, sans valeur d'avis médical ni juridique. Sources primaires citées par fiche. Réservé aux adultes."}}