JP2011513484A5 - - Google Patents
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- JP2011513484A5 JP2011513484A5 JP2010550687A JP2010550687A JP2011513484A5 JP 2011513484 A5 JP2011513484 A5 JP 2011513484A5 JP 2010550687 A JP2010550687 A JP 2010550687A JP 2010550687 A JP2010550687 A JP 2010550687A JP 2011513484 A5 JP2011513484 A5 JP 2011513484A5
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- JP
- Japan
- Prior art keywords
- compound
- receptor
- channel
- voltage
- inhibits
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 150000001875 compounds Chemical class 0.000 claims 49
- 102000005962 receptors Human genes 0.000 claims 27
- 108020003175 receptors Proteins 0.000 claims 27
- 238000000034 method Methods 0.000 claims 26
- 108091006146 Channels Proteins 0.000 claims 18
- -1 AM404 Chemical compound 0.000 claims 16
- 108090000862 Ion Channels Proteins 0.000 claims 15
- 102000004310 Ion Channels Human genes 0.000 claims 15
- 239000012190 activator Substances 0.000 claims 10
- 208000002193 Pain Diseases 0.000 claims 9
- 210000000929 nociceptor Anatomy 0.000 claims 9
- 108091008700 nociceptors Proteins 0.000 claims 9
- BLZVCIGGICSWIG-UHFFFAOYSA-N 2-aminoethoxydiphenylborane Chemical compound C=1C=CC=CC=1B(OCCN)C1=CC=CC=C1 BLZVCIGGICSWIG-UHFFFAOYSA-N 0.000 claims 8
- 208000003251 Pruritus Diseases 0.000 claims 8
- 101000764872 Homo sapiens Transient receptor potential cation channel subfamily A member 1 Proteins 0.000 claims 7
- 102000003610 TRPM8 Human genes 0.000 claims 7
- 102100026186 Transient receptor potential cation channel subfamily A member 1 Human genes 0.000 claims 7
- 101150111302 Trpm8 gene Proteins 0.000 claims 7
- UWYZHKAOTLEWKK-UHFFFAOYSA-N 1,2,3,4-tetrahydroisoquinoline Chemical compound C1=CC=C2CNCCC2=C1 UWYZHKAOTLEWKK-UHFFFAOYSA-N 0.000 claims 6
- VQEONGKQWIFHMN-UHFFFAOYSA-N Nordihydrocapsaicin Chemical compound COC1=CC(CNC(=O)CCCCCC(C)C)=CC=C1O VQEONGKQWIFHMN-UHFFFAOYSA-N 0.000 claims 6
- BLFLLBZGZJTVJG-UHFFFAOYSA-N benzocaine Chemical compound CCOC(=O)C1=CC=C(N)C=C1 BLFLLBZGZJTVJG-UHFFFAOYSA-N 0.000 claims 6
- YKPUWZUDDOIDPM-SOFGYWHQSA-N capsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C\C(C)C)=CC=C1O YKPUWZUDDOIDPM-SOFGYWHQSA-N 0.000 claims 6
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 claims 6
- 229960004919 procaine Drugs 0.000 claims 6
- LEBVLXFERQHONN-UHFFFAOYSA-N 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide Chemical compound CCCCN1CCCCC1C(=O)NC1=C(C)C=CC=C1C LEBVLXFERQHONN-UHFFFAOYSA-N 0.000 claims 5
- QTGIAADRBBLJGA-UHFFFAOYSA-N Articaine Chemical compound CCCNC(C)C(=O)NC=1C(C)=CSC=1C(=O)OC QTGIAADRBBLJGA-UHFFFAOYSA-N 0.000 claims 5
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 claims 5
- 102000003566 TRPV1 Human genes 0.000 claims 5
- 101150016206 Trpv1 gene Proteins 0.000 claims 5
- 229960003831 articaine Drugs 0.000 claims 5
- 229960003150 bupivacaine Drugs 0.000 claims 5
- 229960004194 lidocaine Drugs 0.000 claims 5
- 210000004379 membrane Anatomy 0.000 claims 5
- 239000012528 membrane Substances 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 claims 5
- IITCVPTZKLXSKQ-ZSVIJTOTSA-N 6'-iodoresiniferatoxin Chemical compound C1=C(O)C(OC)=CC(CC(=O)OCC=2C[C@]3(O)C(=O)C(C)=C[C@H]3[C@@]34[C@H](C)C[C@@]5(OC(O4)(CC=4C=CC=CC=4)O[C@@H]5[C@@H]3C=2)C(C)=C)=C1I IITCVPTZKLXSKQ-ZSVIJTOTSA-N 0.000 claims 4
- HGINCPLSRVDWNT-UHFFFAOYSA-N Acrolein Chemical compound C=CC=O HGINCPLSRVDWNT-UHFFFAOYSA-N 0.000 claims 4
- GLZPCOQZEFWAFX-UHFFFAOYSA-N Geraniol Chemical compound CC(C)=CCCC(C)=CCO GLZPCOQZEFWAFX-UHFFFAOYSA-N 0.000 claims 4
- 229920001144 Hydroxy alpha sanshool Polymers 0.000 claims 4
- LHFKHAVGGJJQFF-UEOYEZOQSA-N Hydroxy-alpha-sanshool Chemical compound C\C=C\C=C\C=C/CC\C=C\C(=O)NCC(C)(C)O LHFKHAVGGJJQFF-UEOYEZOQSA-N 0.000 claims 4
- OPZKBPQVWDSATI-KHPPLWFESA-N N-Vanillyloleamide Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)NCC1=CC=C(O)C(OC)=C1 OPZKBPQVWDSATI-KHPPLWFESA-N 0.000 claims 4
- QQBPLXNESPTPNU-KTKRTIGZSA-N N-oleoyldopamine Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)NCCC1=CC=C(O)C(O)=C1 QQBPLXNESPTPNU-KTKRTIGZSA-N 0.000 claims 4
- ROFVXGGUISEHAM-UHFFFAOYSA-N URB597 Chemical compound NC(=O)C1=CC=CC(C=2C=C(OC(=O)NC3CCCCC3)C=CC=2)=C1 ROFVXGGUISEHAM-UHFFFAOYSA-N 0.000 claims 4
- FADFGCOCHHNRHF-VAWYXSNFSA-N [10]-Shogaol Chemical compound CCCCCCCCC\C=C\C(=O)CCC1=CC=C(O)C(OC)=C1 FADFGCOCHHNRHF-VAWYXSNFSA-N 0.000 claims 4
- 210000004027 cell Anatomy 0.000 claims 4
- PFRGXCVKLLPLIP-UHFFFAOYSA-N diallyl disulfide Chemical compound C=CCSSCC=C PFRGXCVKLLPLIP-UHFFFAOYSA-N 0.000 claims 4
- RRAFCDWBNXTKKO-UHFFFAOYSA-N eugenol Chemical compound COC1=CC(CC=C)=CC=C1O RRAFCDWBNXTKKO-UHFFFAOYSA-N 0.000 claims 4
- LHFKHAVGGJJQFF-UHFFFAOYSA-N hydroxyl-alpha-sanshool Natural products CC=CC=CC=CCCC=CC(=O)NCC(C)(C)O LHFKHAVGGJJQFF-UHFFFAOYSA-N 0.000 claims 4
- CDOSHBSSFJOMGT-UHFFFAOYSA-N linalool Chemical compound CC(C)=CCCC(C)(O)C=C CDOSHBSSFJOMGT-UHFFFAOYSA-N 0.000 claims 4
- INWLQCZOYSRPNW-UHFFFAOYSA-N mepivacaine Chemical compound CN1CCCCC1C(=O)NC1=C(C)C=CC=C1C INWLQCZOYSRPNW-UHFFFAOYSA-N 0.000 claims 4
- OGRGWTXWAZBJKF-JXWJAAHMSA-N phorbol 12-phenylacetate 13-acetate 20-homovanillate Chemical compound C1=C(O)C(OC)=CC(CC(=O)OCC=2C[C@]3(O)C(=O)C(C)=C[C@H]3[C@@]3(O)[C@H](C)[C@@H](OC(=O)CC=4C=CC=CC=4)[C@@]4(OC(C)=O)C(C)(C)[C@H]4[C@@H]3C=2)=C1 OGRGWTXWAZBJKF-JXWJAAHMSA-N 0.000 claims 4
- MVFGUOIZUNYYSO-UHFFFAOYSA-N prilocaine Chemical compound CCCNC(C)C(=O)NC1=CC=CC=C1C MVFGUOIZUNYYSO-UHFFFAOYSA-N 0.000 claims 4
- 229960001807 prilocaine Drugs 0.000 claims 4
- 230000001823 pruritic effect Effects 0.000 claims 4
- 229960002372 tetracaine Drugs 0.000 claims 4
- GKCBAIGFKIBETG-UHFFFAOYSA-N tetracaine Chemical compound CCCCNC1=CC=C(C(=O)OCCN(C)C)C=C1 GKCBAIGFKIBETG-UHFFFAOYSA-N 0.000 claims 4
- VLPIATFUUWWMKC-SNVBAGLBSA-N (2r)-1-(2,6-dimethylphenoxy)propan-2-amine Chemical compound C[C@@H](N)COC1=C(C)C=CC=C1C VLPIATFUUWWMKC-SNVBAGLBSA-N 0.000 claims 3
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 claims 3
- 241000723346 Cinnamomum camphora Species 0.000 claims 3
- KEECCEWTUVWFCV-UHFFFAOYSA-N N-acetylprocainamide Chemical compound CCN(CC)CCNC(=O)C1=CC=C(NC(C)=O)C=C1 KEECCEWTUVWFCV-UHFFFAOYSA-N 0.000 claims 3
- FTLDJPRFCGDUFH-UHFFFAOYSA-N Oxethazaine Chemical compound C=1C=CC=CC=1CC(C)(C)N(C)C(=O)CN(CCO)CC(=O)N(C)C(C)(C)CC1=CC=CC=C1 FTLDJPRFCGDUFH-UHFFFAOYSA-N 0.000 claims 3
- KCLANYCVBBTKTO-UHFFFAOYSA-N Proparacaine Chemical compound CCCOC1=CC=C(C(=O)OCCN(CC)CC)C=C1N KCLANYCVBBTKTO-UHFFFAOYSA-N 0.000 claims 3
- 108010025083 TRPV1 receptor Proteins 0.000 claims 3
- NZLBHDRPUJLHCE-UHFFFAOYSA-N aprindine Chemical compound C1C2=CC=CC=C2CC1N(CCCN(CC)CC)C1=CC=CC=C1 NZLBHDRPUJLHCE-UHFFFAOYSA-N 0.000 claims 3
- 229960004957 aprindine Drugs 0.000 claims 3
- 229960005274 benzocaine Drugs 0.000 claims 3
- 229960000846 camphor Drugs 0.000 claims 3
- 229930008380 camphor Natural products 0.000 claims 3
- 229960002504 capsaicin Drugs 0.000 claims 3
- 235000017663 capsaicin Nutrition 0.000 claims 3
- VDANGULDQQJODZ-UHFFFAOYSA-N chloroprocaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1Cl VDANGULDQQJODZ-UHFFFAOYSA-N 0.000 claims 3
- 229960001747 cinchocaine Drugs 0.000 claims 3
- PUFQVTATUTYEAL-UHFFFAOYSA-N cinchocaine Chemical compound C1=CC=CC2=NC(OCCCC)=CC(C(=O)NCCN(CC)CC)=C21 PUFQVTATUTYEAL-UHFFFAOYSA-N 0.000 claims 3
- VNFPBHJOKIVQEB-UHFFFAOYSA-N clotrimazole Chemical compound ClC1=CC=CC=C1C(N1C=NC=C1)(C=1C=CC=CC=1)C1=CC=CC=C1 VNFPBHJOKIVQEB-UHFFFAOYSA-N 0.000 claims 3
- 229960004022 clotrimazole Drugs 0.000 claims 3
- 229960003920 cocaine Drugs 0.000 claims 3
- XJQPQKLURWNAAH-UHFFFAOYSA-N dihydrocapsaicin Chemical compound COC1=CC(CNC(=O)CCCCCCC(C)C)=CC=C1O XJQPQKLURWNAAH-UHFFFAOYSA-N 0.000 claims 3
- RBCYRZPENADQGZ-UHFFFAOYSA-N dihydrocapsaicin Natural products COC1=CC(COC(=O)CCCCCCC(C)C)=CC=C1O RBCYRZPENADQGZ-UHFFFAOYSA-N 0.000 claims 3
- OWQIUQKMMPDHQQ-UHFFFAOYSA-N dimethocaine Chemical compound CCN(CC)CC(C)(C)COC(=O)C1=CC=C(N)C=C1 OWQIUQKMMPDHQQ-UHFFFAOYSA-N 0.000 claims 3
- 229950010160 dimethocaine Drugs 0.000 claims 3
- PJWPNDMDCLXCOM-UHFFFAOYSA-N encainide Chemical compound C1=CC(OC)=CC=C1C(=O)NC1=CC=CC=C1CCC1N(C)CCCC1 PJWPNDMDCLXCOM-UHFFFAOYSA-N 0.000 claims 3
- 229960001142 encainide Drugs 0.000 claims 3
- 229960003404 mexiletine Drugs 0.000 claims 3
- 229960000986 oxetacaine Drugs 0.000 claims 3
- REQCZEXYDRLIBE-UHFFFAOYSA-N procainamide Chemical compound CCN(CC)CCNC(=O)C1=CC=C(N)C=C1 REQCZEXYDRLIBE-UHFFFAOYSA-N 0.000 claims 3
- 229960000244 procainamide Drugs 0.000 claims 3
- 229960003981 proparacaine Drugs 0.000 claims 3
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 claims 2
- 239000001490 (3R)-3,7-dimethylocta-1,6-dien-3-ol Substances 0.000 claims 2
- OQWKEEOHDMUXEO-UHFFFAOYSA-N (6)-shogaol Natural products CCCCCC=CC(=O)CCC1=CC=C(O)C(OC)=C1 OQWKEEOHDMUXEO-UHFFFAOYSA-N 0.000 claims 2
- KJPRLNWUNMBNBZ-QPJJXVBHSA-N (E)-cinnamaldehyde Chemical compound O=C\C=C\C1=CC=CC=C1 KJPRLNWUNMBNBZ-QPJJXVBHSA-N 0.000 claims 2
- CDOSHBSSFJOMGT-JTQLQIEISA-N (R)-linalool Natural products CC(C)=CCC[C@@](C)(O)C=C CDOSHBSSFJOMGT-JTQLQIEISA-N 0.000 claims 2
- ZKMNUMMKYBVTFN-HNNXBMFYSA-N (S)-ropivacaine Chemical compound CCCN1CCCC[C@H]1C(=O)NC1=C(C)C=CC=C1C ZKMNUMMKYBVTFN-HNNXBMFYSA-N 0.000 claims 2
- WEEGYLXZBRQIMU-UHFFFAOYSA-N 1,8-cineole Natural products C1CC2CCC1(C)OC2(C)C WEEGYLXZBRQIMU-UHFFFAOYSA-N 0.000 claims 2
- AWJJLYZBWRIBCZ-UGTJMOTHSA-N 3'-O-(4-Benzoyl)benzoyl ATP Chemical compound O([C@@H]1[C@@H](COP(O)(=O)OP(O)(=O)OP(O)(O)=O)O[C@H]([C@@H]1O)N1C=2N=CN=C(C=2N=C1)N)C(=O)C(C=C1)=CC=C1C(=O)C1=CC=CC=C1 AWJJLYZBWRIBCZ-UGTJMOTHSA-N 0.000 claims 2
- HQFWVSGBVLEQGA-UHFFFAOYSA-N 4-aminobenzoic acid 3-(dibutylamino)propyl ester Chemical compound CCCCN(CCCC)CCCOC(=O)C1=CC=C(N)C=C1 HQFWVSGBVLEQGA-UHFFFAOYSA-N 0.000 claims 2
- 102100027782 ATP synthase-coupling factor 6, mitochondrial Human genes 0.000 claims 2
- NPBVQXIMTZKSBA-UHFFFAOYSA-N Chavibetol Natural products COC1=CC=C(CC=C)C=C1O NPBVQXIMTZKSBA-UHFFFAOYSA-N 0.000 claims 2
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims 2
- VTUSIVBDOCDNHS-UHFFFAOYSA-N Etidocaine Chemical compound CCCN(CC)C(CC)C(=O)NC1=C(C)C=CC=C1C VTUSIVBDOCDNHS-UHFFFAOYSA-N 0.000 claims 2
- WEEGYLXZBRQIMU-WAAGHKOSSA-N Eucalyptol Chemical compound C1C[C@H]2CC[C@]1(C)OC2(C)C WEEGYLXZBRQIMU-WAAGHKOSSA-N 0.000 claims 2
- 239000005770 Eugenol Substances 0.000 claims 2
- IKYCZSUNGFRBJS-UHFFFAOYSA-N Euphorbia factor RL9 = U(1) = Resiniferatoxin Natural products COC1=CC(O)=CC(CC(=O)OCC=2CC3(O)C(=O)C(C)=CC3C34C(C)CC5(OC(O4)(CC=4C=CC=CC=4)OC5C3C=2)C(C)=C)=C1 IKYCZSUNGFRBJS-UHFFFAOYSA-N 0.000 claims 2
- 239000005792 Geraniol Substances 0.000 claims 2
- GLZPCOQZEFWAFX-YFHOEESVSA-N Geraniol Natural products CC(C)=CCC\C(C)=C/CO GLZPCOQZEFWAFX-YFHOEESVSA-N 0.000 claims 2
- 101000936965 Homo sapiens ATP synthase-coupling factor 6, mitochondrial Proteins 0.000 claims 2
- 102000003820 Lipoxygenases Human genes 0.000 claims 2
- 108090000128 Lipoxygenases Proteins 0.000 claims 2
- CAJIGINSTLKQMM-UHFFFAOYSA-N Propoxycaine Chemical compound CCCOC1=CC(N)=CC=C1C(=O)OCCN(CC)CC CAJIGINSTLKQMM-UHFFFAOYSA-N 0.000 claims 2
- UVMRYBDEERADNV-UHFFFAOYSA-N Pseudoeugenol Natural products COC1=CC(C(C)=C)=CC=C1O UVMRYBDEERADNV-UHFFFAOYSA-N 0.000 claims 2
- 102000002294 Purinergic P2X Receptors Human genes 0.000 claims 2
- 108010000836 Purinergic P2X Receptors Proteins 0.000 claims 2
- 102000016913 Voltage-Gated Sodium Channels Human genes 0.000 claims 2
- 108010053752 Voltage-Gated Sodium Channels Proteins 0.000 claims 2
- WSINRQSTSKCAEN-UGTJMOTHSA-N [(2r,3r,4r,5r)-2-(6-aminopurin-9-yl)-4-hydroxy-5-[[hydroxy-[hydroxy(phosphonooxy)phosphoryl]oxyphosphoryl]oxymethyl]oxolan-3-yl] 4-benzoylbenzoate Chemical compound O([C@@H]1[C@H](O)[C@@H](COP(O)(=O)OP(O)(=O)OP(O)(O)=O)O[C@H]1N1C=2N=CN=C(C=2N=C1)N)C(=O)C(C=C1)=CC=C1C(=O)C1=CC=CC=C1 WSINRQSTSKCAEN-UGTJMOTHSA-N 0.000 claims 2
- KDYVIORLSJSMTG-UHFFFAOYSA-N [2-[(3,4-dimethylphenyl)methyl]-3-[(4-hydroxy-3-methoxyphenyl)methylcarbamothioylamino]propyl] 2,2-dimethylpropanoate Chemical compound C1=C(O)C(OC)=CC(CNC(=S)NCC(COC(=O)C(C)(C)C)CC=2C=C(C)C(C)=CC=2)=C1 KDYVIORLSJSMTG-UHFFFAOYSA-N 0.000 claims 2
- XNOBOKJVOTYSJV-KQYNXXCUSA-N [[(2r,3s,4r,5r)-5-(6-amino-2-methylsulfanylpurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate Chemical compound C12=NC(SC)=NC(N)=C2N=CN1[C@@H]1O[C@H](COP(O)(=O)OP(O)(=O)OP(O)(O)=O)[C@@H](O)[C@H]1O XNOBOKJVOTYSJV-KQYNXXCUSA-N 0.000 claims 2
- AYJBWCXXFCSXNE-UHFFFAOYSA-N [hydroxy(phosphonooxy)phosphinothioyl] dihydrogen phosphate Chemical compound OP(O)(=O)OP(O)(=S)OP(O)(O)=O AYJBWCXXFCSXNE-UHFFFAOYSA-N 0.000 claims 2
- ZOJBYZNEUISWFT-UHFFFAOYSA-N allyl isothiocyanate Chemical compound C=CCN=C=S ZOJBYZNEUISWFT-UHFFFAOYSA-N 0.000 claims 2
- LGEQQWMQCRIYKG-DOFZRALJSA-N anandamide Chemical compound CCCCC\C=C/C\C=C/C\C=C/C\C=C/CCCC(=O)NCCO LGEQQWMQCRIYKG-DOFZRALJSA-N 0.000 claims 2
- LGEQQWMQCRIYKG-UHFFFAOYSA-N arachidonic acid ethanolamide Natural products CCCCCC=CCC=CCC=CCC=CCCCC(=O)NCCO LGEQQWMQCRIYKG-UHFFFAOYSA-N 0.000 claims 2
- 229960003369 butacaine Drugs 0.000 claims 2
- 229960002023 chloroprocaine Drugs 0.000 claims 2
- 229960005233 cineole Drugs 0.000 claims 2
- 229940117916 cinnamic aldehyde Drugs 0.000 claims 2
- KJPRLNWUNMBNBZ-UHFFFAOYSA-N cinnamic aldehyde Natural products O=CC=CC1=CC=CC=C1 KJPRLNWUNMBNBZ-UHFFFAOYSA-N 0.000 claims 2
- 239000010630 cinnamon oil Substances 0.000 claims 2
- 239000010634 clove oil Substances 0.000 claims 2
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 2
- 235000018417 cysteine Nutrition 0.000 claims 2
- 235000014113 dietary fatty acids Nutrition 0.000 claims 2
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims 2
- 229960003976 etidocaine Drugs 0.000 claims 2
- 229960002217 eugenol Drugs 0.000 claims 2
- 229930195729 fatty acid Natural products 0.000 claims 2
- 239000000194 fatty acid Substances 0.000 claims 2
- 150000004665 fatty acids Chemical class 0.000 claims 2
- 229940113087 geraniol Drugs 0.000 claims 2
- JZLXEKNVCWMYHI-UHFFFAOYSA-N gingerol Natural products CCCCC(O)CC(=O)CCC1=CC=C(O)C(OC)=C1 JZLXEKNVCWMYHI-UHFFFAOYSA-N 0.000 claims 2
- 235000002780 gingerol Nutrition 0.000 claims 2
- WPFVBOQKRVRMJB-UHFFFAOYSA-N hydroxycitronellal Chemical compound O=CCC(C)CCCC(C)(C)O WPFVBOQKRVRMJB-UHFFFAOYSA-N 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 2
- 229960004288 levobupivacaine Drugs 0.000 claims 2
- LEBVLXFERQHONN-INIZCTEOSA-N levobupivacaine Chemical compound CCCCN1CCCC[C@H]1C(=O)NC1=C(C)C=CC=C1C LEBVLXFERQHONN-INIZCTEOSA-N 0.000 claims 2
- 229930007744 linalool Natural products 0.000 claims 2
- 229940041616 menthol Drugs 0.000 claims 2
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 claims 2
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 claims 2
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 claims 2
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 claims 2
- 239000008164 mustard oil Substances 0.000 claims 2
- 210000002569 neuron Anatomy 0.000 claims 2
- OPZKBPQVWDSATI-UHFFFAOYSA-N oleoyl vanillylamide Natural products CCCCCCCCC=CCCCCCCCC(=O)NCC1=CC=C(O)C(OC)=C1 OPZKBPQVWDSATI-UHFFFAOYSA-N 0.000 claims 2
- 229950010717 olvanil Drugs 0.000 claims 2
- MXXWOMGUGJBKIW-YPCIICBESA-N piperine Chemical compound C=1C=C2OCOC2=CC=1/C=C/C=C/C(=O)N1CCCCC1 MXXWOMGUGJBKIW-YPCIICBESA-N 0.000 claims 2
- 229940075559 piperine Drugs 0.000 claims 2
- WVWHRXVVAYXKDE-UHFFFAOYSA-N piperine Natural products O=C(C=CC=Cc1ccc2OCOc2c1)C3CCCCN3 WVWHRXVVAYXKDE-UHFFFAOYSA-N 0.000 claims 2
- 235000019100 piperine Nutrition 0.000 claims 2
- 108090000765 processed proteins & peptides Proteins 0.000 claims 2
- 229950003255 propoxycaine Drugs 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
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| WO2010085589A2 (en) | 2009-01-22 | 2010-07-29 | G&H Brands Llc | Desensitizing drug product |
| EP2451944A4 (en) * | 2009-07-10 | 2012-11-28 | Harvard College | PERMANENTLY CHARGED SODIUM AND CALCIUM CHANNEL BLOCKERS AS ANTI-INFLAMMATORY AGENTS |
| JP5832856B2 (ja) * | 2010-12-15 | 2015-12-16 | 久光製薬株式会社 | 局所鎮痛作用増強剤及び局所鎮痛キット |
| EP3363437B8 (en) | 2011-02-18 | 2021-11-03 | Endo Pharmaceuticals Inc. | Aminoindane compounds and use thereof in treating pain |
| DK2771320T3 (en) | 2011-10-24 | 2016-10-03 | Endo Pharmaceuticals Inc | Cyclohexylamines |
| US8779003B2 (en) | 2011-12-29 | 2014-07-15 | Mackay Memorial Hospital | Method and composition for prolonging analgesic effect of local anesthetic |
| WO2014028675A1 (en) | 2012-08-15 | 2014-02-20 | Endo Pharmaceuticals Inc. | Use of aminoindane compounds in treating overactive bladder and interstitial cystitis |
| ES2831028T3 (es) | 2013-02-08 | 2021-06-07 | Gen Mills Inc | Productos alimenticios reducidos en sodio |
| AU2015247815A1 (en) * | 2014-04-14 | 2016-11-03 | Flex Pharma, Inc. | Ion channel activators and methods of use |
| JP6833811B2 (ja) | 2015-08-03 | 2021-02-24 | プレジデント アンド フェローズ オブ ハーバード カレッジ | 荷電イオンチャネル遮断薬及び使用方法 |
| CN106214678B (zh) * | 2016-07-26 | 2020-12-29 | 上海璃道医药科技有限公司 | 苯酮类药物的用途 |
| WO2018136943A1 (en) | 2017-01-23 | 2018-07-26 | Flex Pharma, Inc. | Compositions and methods affecting exercise performance |
| KR101877002B1 (ko) * | 2017-03-06 | 2018-07-12 | 서울대학교 산학협력단 | 피라졸 유도체를 유효성분으로 함유하는 소양증의 예방 또는 치료용 약학적 조성물 및 이를 검출하기 위한 스크리닝 방법 |
| KR101867779B1 (ko) * | 2017-12-08 | 2018-06-19 | 서울대학교산학협력단 | 피라졸 유도체를 유효성분으로 함유하는 소양증의 예방 또는 치료용 약학적 조성물 및 이를 검출하기 위한 스크리닝 방법 |
| WO2019144139A1 (en) * | 2018-01-22 | 2019-07-25 | Oregon State University | Immunogenic compositions comprising mycobacterium bovis surface proteins and uses thereof |
| EP3762034B1 (en) | 2018-03-05 | 2025-08-27 | Wylder Nation Foundation | A fatty acid amide hydrolase (faahi) inhibitor for use in inhibiting the cellular accumulation of a sphingolipid in a subject that has lysosomal storage disease or disorder |
| WO2020035555A2 (en) * | 2018-08-15 | 2020-02-20 | Pharmacyl Ab | Substituted benzamides and their use in therapy |
| CN109498604A (zh) * | 2018-12-24 | 2019-03-22 | 复旦大学 | 香叶醇新用途，预防和治疗非疾病引起的瘙痒症的配制品及方法 |
| CN113924094A (zh) | 2019-03-11 | 2022-01-11 | 诺西恩医疗公司 | 酯取代的离子通道阻滞剂及其使用方法 |
| US10780083B1 (en) | 2019-03-11 | 2020-09-22 | Nocion Therapeutics, Inc. | Charged ion channel blockers and methods for use |
| EP3937929A4 (en) | 2019-03-11 | 2022-12-28 | Nocion Therapeutics, Inc. | CHARGED ION CHANNEL BLOCKERS AND METHODS OF USE |
| US10828287B2 (en) | 2019-03-11 | 2020-11-10 | Nocion Therapeutics, Inc. | Charged ion channel blockers and methods for use |
| WO2020185881A1 (en) | 2019-03-11 | 2020-09-17 | Nocion Therapeutics, Inc. | Charged ion channel blockers and methods for use |
| BR112022008575A2 (pt) | 2019-11-06 | 2022-08-09 | Nocion Therapeutics Inc | Bloqueadores de canal iônico carregado e métodos para uso |
| EP4054586A4 (en) | 2019-11-06 | 2023-11-22 | Nocion Therapeutics, Inc. | Charged ion channel blockers and methods for use |
| US20230165812A1 (en) * | 2020-02-27 | 2023-06-01 | President And Fellows Of Harvard College | Nociceptor neurons control cancer immunosurveillance |
| JP2023515874A (ja) * | 2020-03-04 | 2023-04-14 | ノイキュアズ，インコーポレーテッド | Ｔｒｐｖ１調節物質の投与に関連する交感神経興奮を防止するためのｑｘ３１４の使用 |
| US12162851B2 (en) | 2020-03-11 | 2024-12-10 | Nocion Therapeutics, Inc. | Charged ion channel blockers and methods for use |
| KR20230022830A (ko) | 2020-03-11 | 2023-02-16 | 녹시온 테라퓨틱스 인코포레이티드 | 하전된 이온 채널 차단제 및 사용 방법 |
| CN113509457B (zh) * | 2020-09-07 | 2023-03-21 | 四川昇嘉科技有限公司 | 山椒素在制备治疗湿疹的药物中的用途 |
| US11977085B1 (en) | 2023-09-05 | 2024-05-07 | Elan Ehrlich | Date rape drug detection device and method of using same |
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| US6413961B1 (en) * | 1995-12-12 | 2002-07-02 | Omeros Medical Systems, Inc. | Irrigation solution and method for inhibition of pain and inflammation |
| JP2003516966A (ja) * | 1999-12-15 | 2003-05-20 | ユーシィービィ ファルチム ソシエテアノニム | 環状４級アンモニウム化合物 |
| CA2446060A1 (en) * | 2001-05-07 | 2002-11-14 | Corium International | Compositions and delivery systems for administration of a local anesthetic agent |
| US7943166B2 (en) * | 2003-04-10 | 2011-05-17 | Neurogesx, Inc. | Methods and compositions for administration of TRPV1 agonists |
| ES2223277B1 (es) * | 2003-06-19 | 2006-03-01 | Fernando Bouffard Fita | Composicion anestesica para administracion topica. |
| AU2005210637B2 (en) * | 2004-01-30 | 2010-09-16 | A.V. Topchiev Institute Of Petrochemical Synthesis | Rapidly dissolving film for delivery of an active agent |
| EP1763370B1 (en) * | 2004-06-02 | 2015-04-29 | NeurogesX Inc. | Formulations comprising capsaicin, a local anesthetic and/or an antipruritic agent for the treatment of pain |
| US20100099772A1 (en) * | 2006-11-20 | 2010-04-22 | Bean Bruce P | Methods, compositions, and kits for treating pain and pruritis |
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