{"schemaVersion":"cwiki-fiche-1.0","identifiers":{"inchiKey":"BHBOSTKQCZEAJM-UHFFFAOYSA-N","prefName":"JNJ-1661010","symbol":"JNJ-1661010","iupacName":"N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide","aliases":["JNJ-1661010","JNJ1661010"],"cas":null,"pubchemCid":"2809273","chebiId":null,"smiles":"C1CN(CCN1C2=NC(=NS2)C3=CC=CC=C3)C(=O)NC4=CC=CC=C4","molecularFormula":"C19H19N5OS","molecularWeight":365.5,"xrefs":{"pubchem":"https://pubchem.ncbi.nlm.nih.gov/compound/2809273"}},"classification":{"family":"ecs_tool","familyLabel":"ECS modulator (research)","origin":"synthetic","originLabel":"Synthétique","structuralClassFr":null},"originSynthesis":{"heading":"Origin (research tool)","summaryFr":"No biosynthetic pathway: a chemically synthesised molecule of the aryl piperazine urea class, carrying a 1,2,4-thiadiazole ring.","originNote":"Fully synthetic molecule, from pharmaceutical chemistry work on FAAH inhibitors. The reference data used for this entry record no natural occurrence, either in hemp or in any other living organism.","discovered":""},"pharmacology":{"summaryFr":"JNJ-1661010 is an inhibitor of FAAH, the enzyme that breaks down anandamide and other fatty acid amides. Described in 2008 in a medicinal chemistry series, then characterised in 2009 by pharmacology work carried out at Johnson & Johnson, the molecule forms a covalent bond with the enzyme that slowly breaks down. In rats, it raises brain levels of anandamide, OEA and PEA and reduces experimental pain of neuropathic, inflammatory and acute origin (Karbarz et al., 2009). Other work in mice reports a reduction of spontaneous contractions of isolated uterus, an attenuation of haloperidol-induced catalepsy and an amelioration of collagen-induced arthritis (Pagano et al., 2017; Celorrio et al., 2016; Lowin et al., 2015). The data are exclusively preclinical: no therapeutic indication is established and no human clinical data were identified in the sources consulted.","receptorSummaryFr":"FAAH inhibitor, the enzyme that breaks down anandamide and other fatty acid amides, through a mechanism based on the enzyme: the molecule forms a covalent bond with it, which slowly breaks down. The IC50 is 33 nM against human FAAH after 20 minutes of preincubation, and 12 nM after 60 minutes (Keith et al., 2008). It is more than 100-fold more selective for FAAH-1 than for FAAH-2 (Karbarz et al., 2009). No affinity constant for CB1 or CB2 is published in the sources consulted for this entry.","binding":[{"target":"FAAH","efficacy":"modulator","relativeActivity":75,"reported":"CI50 33 nM sur FAAH humaine après 20 min de préincubation (Keith et coll., 2008)","confidence":"medium"}],"references":[{"label":"Keith et coll., Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase, Bioorganic & Medicinal Chemistry Letters, 2008","pmid":"18693015","doi":"10.1016/j.bmcl.2008.07.081","url":"https://pubmed.ncbi.nlm.nih.gov/18693015/"},{"label":"Karbarz et coll., Biochemical and biological properties of 4-(3-phenyl-[1,2,4]thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase, Anesthesia and Analgesia, 2009","pmid":"19095868","doi":"10.1213/ane.0b013e31818c7cbd","url":"https://pubmed.ncbi.nlm.nih.gov/19095868/"},{"label":"Palermo et coll., Covalent inhibitors of fatty acid amide hydrolase: a rationale for the activity of piperidine and piperazine aryl ureas, Journal of Medicinal Chemistry, 2011","pmid":"21830831","doi":"10.1021/jm2004283","url":"https://pubmed.ncbi.nlm.nih.gov/21830831/"},{"label":"Lowin et coll., Anti-inflammatory effects of N-acylethanolamines in rheumatoid arthritis synovial cells, Arthritis Research & Therapy, 2015","pmid":"26567045","doi":"10.1186/s13075-015-0845-5","url":"https://pubmed.ncbi.nlm.nih.gov/26567045/"},{"label":"Celorrio et coll., Fatty acid amide hydrolase inhibition for the symptomatic relief of Parkinson's disease, Brain, Behavior, and Immunity, 2016","pmid":"27318096","doi":"10.1016/j.bbi.2016.06.010","url":"https://pubmed.ncbi.nlm.nih.gov/27318096/"},{"label":"Pagano et coll., Role of the endocannabinoid system in the control of mouse myometrium contractility during the menstrual cycle, Biochemical Pharmacology, 2017","pmid":"27899300","doi":"10.1016/j.bcp.2016.11.023","url":"https://pubmed.ncbi.nlm.nih.gov/27899300/"},{"label":"ChEMBL, fiche composé CHEMBL460273 (activités FAAH et paramètres rat tirés de Keith et coll., 2008)","pmid":null,"doi":null,"url":"https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL460273/"},{"label":"PubChem, CID 2809273 (JNJ-1661010)","pmid":null,"doi":null,"url":"https://pubchem.ncbi.nlm.nih.gov/compound/2809273"},{"label":"ANSM, liste consolidée des stupéfiants (mise à jour du 16 février 2026)","pmid":null,"doi":null,"url":"https://ansm.sante.fr/uploads/2026/02/17/20260217-stupefiants-liste-consolidee.pdf"},{"label":"INCB, Green List 2026 (Conventions de 1961 et 1971)","pmid":null,"doi":null,"url":"https://www.incb.org/incb/uploads/documents/Psychotropics/forms/greenlist/2026/2510307E.pdf"}]},"pharmacokinetics":null,"metabolism":null,"detection":null,"subjectiveEffects":{"profile":[{"key":"calm","label":"Calm","description":"Relaxation of body and mind; reduced mental noise without marked drowsiness.","intensity":5},{"key":"focus","label":"Clarity","description":"Sustained attention and clear thinking; functional lucidity, not euphoria.","intensity":5},{"key":"sleep","label":"Sleep","description":"Sedative effect: aids sleep onset and the continuity of deep sleep.","intensity":5},{"key":"appetite","label":"Appetite","description":"Stimulation of hunger and of taste appreciation (the “munchies” effect).","intensity":5},{"key":"uplift","label":"High","description":"Euphoria and sensory intensity; altered perception of time and space.","intensity":5}],"doseRanges":null,"humanDataCharacterised":false},"indications":{"approvedMedicines":[]},"harmProfile":{"unstudiedBanner":true,"bannerTextFr":"Aucune dose humaine caractérisée : données animales / in vitro uniquement. Profil d'effet, marge de sécurité et toxicité aiguë non documentés en clinique humaine.","toxicologyFr":null},"legal":{"scheduleStatus":"unscheduled","scheduleLabel":"Unscheduled","frScheduleStatus":"unscheduled","tiers":[{"jurisdiction":"international","jurisdictionLabel":"International","label":null,"reference":null,"url":null,"effectiveDate":null,"lastVerified":"2026-05-01","supersededBy":null},{"jurisdiction":"eu","jurisdictionLabel":"Union européenne","label":"Not listed in the 1961 and 1971 international conventions (INCB Green List, 2026 edition). No harmonised control measure at European Union level was identified in the sources consulted for this entry: the status therefore falls under the national law of each member state.","reference":null,"url":null,"effectiveDate":null,"lastVerified":"2026-05-01","supersededBy":null},{"jurisdiction":"fr","jurisdictionLabel":"France","label":"Not named in the consolidated list of narcotics published by ANSM (update of 16 February 2026), either under its code or its chemical name; its structure meets none of the generic family definitions of that list (notably indole and indazole methanones, carboxylates and carboxamides, naphthoylpyrroles, naphthylmethylindoles, naphthylidene indenes, cyclohexylphenols, pyrrolo[3,2-c]pyridine carboxamides and thiazolyl indoles), nor the clauses covering benzofurans, cathinones or phenethylamines. Not classified in France on that basis, subject to legal review.","reference":null,"url":null,"effectiveDate":null,"lastVerified":"2026-05-01","supersededBy":null}],"sourcesFr":"EUR-Lex, UNODC, CND, ANSM, IUPHAR/BPS, ChEBI, EUDA."},"references":[{"label":"Keith et coll., Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase, Bioorganic & Medicinal Chemistry Letters, 2008","pmid":"18693015","doi":"10.1016/j.bmcl.2008.07.081","url":"https://pubmed.ncbi.nlm.nih.gov/18693015/"},{"label":"Karbarz et coll., Biochemical and biological properties of 4-(3-phenyl-[1,2,4]thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase, Anesthesia and Analgesia, 2009","pmid":"19095868","doi":"10.1213/ane.0b013e31818c7cbd","url":"https://pubmed.ncbi.nlm.nih.gov/19095868/"},{"label":"Palermo et coll., Covalent inhibitors of fatty acid amide hydrolase: a rationale for the activity of piperidine and piperazine aryl ureas, Journal of Medicinal Chemistry, 2011","pmid":"21830831","doi":"10.1021/jm2004283","url":"https://pubmed.ncbi.nlm.nih.gov/21830831/"},{"label":"Lowin et coll., Anti-inflammatory effects of N-acylethanolamines in rheumatoid arthritis synovial cells, Arthritis Research & Therapy, 2015","pmid":"26567045","doi":"10.1186/s13075-015-0845-5","url":"https://pubmed.ncbi.nlm.nih.gov/26567045/"},{"label":"Celorrio et coll., Fatty acid amide hydrolase inhibition for the symptomatic relief of Parkinson's disease, Brain, Behavior, and Immunity, 2016","pmid":"27318096","doi":"10.1016/j.bbi.2016.06.010","url":"https://pubmed.ncbi.nlm.nih.gov/27318096/"},{"label":"Pagano et coll., Role of the endocannabinoid system in the control of mouse myometrium contractility during the menstrual cycle, Biochemical Pharmacology, 2017","pmid":"27899300","doi":"10.1016/j.bcp.2016.11.023","url":"https://pubmed.ncbi.nlm.nih.gov/27899300/"},{"label":"ChEMBL, fiche composé CHEMBL460273 (activités FAAH et paramètres rat tirés de Keith et coll., 2008)","pmid":null,"doi":null,"url":"https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL460273/"},{"label":"PubChem, CID 2809273 (JNJ-1661010)","pmid":null,"doi":null,"url":"https://pubchem.ncbi.nlm.nih.gov/compound/2809273"},{"label":"ANSM, liste consolidée des stupéfiants (mise à jour du 16 février 2026)","pmid":null,"doi":null,"url":"https://ansm.sante.fr/uploads/2026/02/17/20260217-stupefiants-liste-consolidee.pdf"},{"label":"INCB, Green List 2026 (Conventions de 1961 et 1971)","pmid":null,"doi":null,"url":"https://www.incb.org/incb/uploads/documents/Psychotropics/forms/greenlist/2026/2510307E.pdf"}],"meta":{"slug":"jnj-1661010","url":"https://en.phytogrammes.com/wiki/jnj-1661010","lastVerified":"2026-05-01","dataUpdatedAt":"2026-10-13","confidence":"high","dataCompletenessPct":90,"disclaimerFr":"Contenu éditorial informatif, sans valeur d'avis médical ni juridique. Sources primaires citées par fiche. Réservé aux adultes."}}