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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| US8637577B2 (en) | 2009-01-22 | 2014-01-28 | Absorption Pharmaceuticals, LLC | Desensitizing drug product |
| JP6205133B2 (ja) * | 2009-07-10 | 2017-09-27 | 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 | 抗炎症剤としての恒久的に荷電したナトリウムおよびカルシウムチャンネルブロッカー |
| 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 |
| US8865741B2 (en) | 2011-02-18 | 2014-10-21 | Asana Biosciences, Llc | Aminoindane compounds and use thereof in treating pain |
| EP2771320B1 (en) | 2011-10-24 | 2016-06-22 | 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 |
| CN111557432B (zh) | 2013-02-08 | 2023-08-04 | 通用磨坊公司 | 低钠食品 |
| EA201692060A1 (ru) * | 2014-04-14 | 2017-02-28 | Флекс Фарма, Инк. | Активаторы ионного канала и способы их применения |
| RU2018107695A (ru) | 2015-08-03 | 2019-09-05 | Президент Энд Феллоуз Оф Гарвард Колледж | Заряженные блокаторы ионных каналов и способы их применения |
| 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 |
| WO2019173394A1 (en) | 2018-03-05 | 2019-09-12 | Wylder Nation Foundation | Compositions and methods for activating signaling through the cb1 cannabinoid receptor for treating and preventing diseases and disorders characterized by abnormal cellular accumulation of sphingolipids such as sphingomyelin |
| MX2021001351A (es) * | 2018-08-15 | 2021-04-13 | Pharmacyl Ab | Benzamidas sustituidas y su uso en terapia. |
| 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 |
| BR112021017809A2 (pt) | 2019-03-11 | 2021-11-23 | Nocion Therapeutics Inc | Bloqueadores de canais iônicos substituídos por éster e métodos para uso |
| US10786485B1 (en) | 2019-03-11 | 2020-09-29 | Nocion Therapeutics, Inc. | Charged ion channel blockers and methods for use |
| JP7692834B2 (ja) | 2019-03-11 | 2025-06-16 | ノシオン セラピューティクス，インコーポレイテッド | 荷電したイオンチャンネル遮断薬および使用方法 |
| BR112021017772A2 (pt) | 2019-03-11 | 2021-11-16 | Nocion Therapeutics Inc | Bloqueadores de canais de íons carregados e métodos para uso |
| US10780083B1 (en) | 2019-03-11 | 2020-09-22 | Nocion Therapeutics, Inc. | Charged ion channel blockers and methods for use |
| JP7513713B2 (ja) | 2019-11-06 | 2024-07-09 | ノシオン セラピューティクス，インコーポレイテッド | 荷電したイオンチャンネル遮断薬および使用方法 |
| AU2020380118A1 (en) | 2019-11-06 | 2022-05-19 | 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 |
| BR112022017801A2 (pt) | 2020-03-11 | 2022-10-25 | Nocion Therapeutics Inc | Bloqueadores de canais de íons carregados e métodos para uso |
| 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 |
| AU2334501A (en) * | 1999-12-15 | 2001-06-25 | Ucb Farchim Sa | Cyclic quaternary ammonium compounds |
| US20030027833A1 (en) * | 2001-05-07 | 2003-02-06 | Cleary Gary W. | Compositions and delivery systems for administration of a local anesthetic agent |
| EA012599B1 (ru) * | 2003-04-10 | 2009-10-30 | Ньюроджескс, Инк. | Способы и композиции для введения агонистов trpv1 |
| ES2223277B1 (es) * | 2003-06-19 | 2006-03-01 | Fernando Bouffard Fita | Composicion anestesica para administracion topica. |
| CN102764247B (zh) * | 2004-01-30 | 2016-04-20 | 考里安国际公司 | 递送活性剂的快速溶解膜 |
| ES2542847T3 (es) * | 2004-06-02 | 2015-08-12 | Neurogesx Inc. | Formulaciones que comprenden capsaicina, un anestésico local y/o un agente antipruriginoso para el tratamiento del dolor |
| JP2010510227A (ja) * | 2006-11-20 | 2010-04-02 | プレジデント アンド フェロウズ オブ ハーバード カレッジ | 痛みおよび痒みの治療方法、組成物およびキット |
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