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Nociceptive sensory peripheral neurons often express both heat sensitive (VR1) and cold-sensitive (CMR1 (rat), TRPM8 (human)) receptors that are part of the transient receptor potential (TRP) superfamily. Icilin is a synthetic CMR1/TRPM8 super agonist that is 2.5-fold more efficacious and nearly 200-fold more potent than the reference cold thermosensory agonist, l-menthol. Icilin induces sensations of intense cold when applied orally in humans, and induces 'wet dog shakes', a behavioral marker of cold sensation, when given to rats. Icilin should serve as the reference cold nociceptive agonist for TRP-type ion channels in the future.Formal Name: 3,6-dihydro-1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-2(1H)-pyrimidinone. CAS Number: 36945-98-9. Synonyms: AG 3-5. Molecular Formula: C16H13N3O4. Formula Weight: 311.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 25 mg/ml, DMSO:PBS (pH 7.2) (1:5): 0.1 mg/ml. SMILES: O=C1N([H])C(C2=CC([N+]([O-])=O)=CC=C2)=CCN1C3=CC=CC=C3O. InChi Code: InChI=1S/C16H13N3O4/c20-15-7-2-1-6-14(15)18-9-8-13(17-16(18)21)11-4-3-5-12(10-11)19(22)23/h1-8,10,20H,9H2,(H,17,21). InChi Key: RCEFMOGVOYEGJN-UHFFFAOYSA-N.
Keywords:
AG 3-5, 3,6-dihydro-1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-2(1H)-pyrimidinone
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