The Experts below are selected from a list of 84 Experts worldwide ranked by ideXlab platform
Masashi Deguchi - One of the best experts on this subject based on the ideXlab platform.
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discovery of s 444823 a potent cb1 cb2 dual agonist as an Antipruritic Agent
Bioorganic & Medicinal Chemistry Letters, 2012Co-Authors: Masahide Odan, Yoshiharu Hiramatsu, Masanao Inagaki, Hiroshi Hashizume, Yasuhiko Fujii, Susumu Mitsumori, Natsuki Ishizuka, Yasuhide Morioka, Masahiko Soga, Masashi DeguchiAbstract:Abstract The optimization of a series of 3-carbamoyl 2-pyridone derivatives as CB agonists is reported. These efforts resulted in the discovery of 3-(2-(1-(cyclohexylmethyl)-2-oxo-1,2,5,6,7,8,9,10-octahydrocycloocta[b]pyridine-3-carboxamido)thiazol-4-yl)propanoic acid ( 21 ), a potent dual CB1/CB2 agonist without CNS side effects induced by CB1 receptor activation. It exhibited strong inhibition of scratching as a 1.0% acetone solution in the pruritic model.
Yoshiharu Hiramatsu - One of the best experts on this subject based on the ideXlab platform.
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discovery of s 777469 an orally available cb2 agonist as an Antipruritic Agent
Bioorganic & Medicinal Chemistry Letters, 2012Co-Authors: Masahide Odan, Natsuki Ishizuka, Yoshiharu Hiramatsu, Masanao Inagaki, Hiroshi Hashizume, Yasuhiko Fujii, Susumu Mitsumori, Yasuhide Morioka, Masahiko Soga, Masashi DeguchiAbstract:Abstract The discovery of novel CB2 ligands based on the 3-carbamoyl-2-pyridone derivatives by adjusting the size of side chain at 1-, 5- and 6-position is reported. The structure–activity relationship around this template lead to the identification of S-777469 as a selective CB2 receptor agonist, which exhibited the significant inhibition of scratching induced by Compound 48/80 at 1.0 mg/kg po and 10 mg/kg po (55% and 61%, respectively).
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discovery of s 444823 a potent cb1 cb2 dual agonist as an Antipruritic Agent
Bioorganic & Medicinal Chemistry Letters, 2012Co-Authors: Masahide Odan, Yoshiharu Hiramatsu, Masanao Inagaki, Hiroshi Hashizume, Yasuhiko Fujii, Susumu Mitsumori, Natsuki Ishizuka, Yasuhide Morioka, Masahiko Soga, Masashi DeguchiAbstract:Abstract The optimization of a series of 3-carbamoyl 2-pyridone derivatives as CB agonists is reported. These efforts resulted in the discovery of 3-(2-(1-(cyclohexylmethyl)-2-oxo-1,2,5,6,7,8,9,10-octahydrocycloocta[b]pyridine-3-carboxamido)thiazol-4-yl)propanoic acid ( 21 ), a potent dual CB1/CB2 agonist without CNS side effects induced by CB1 receptor activation. It exhibited strong inhibition of scratching as a 1.0% acetone solution in the pruritic model.
Hiroshi Hashizume - One of the best experts on this subject based on the ideXlab platform.
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discovery of s 777469 an orally available cb2 agonist as an Antipruritic Agent
Bioorganic & Medicinal Chemistry Letters, 2012Co-Authors: Masahide Odan, Natsuki Ishizuka, Yoshiharu Hiramatsu, Masanao Inagaki, Hiroshi Hashizume, Yasuhiko Fujii, Susumu Mitsumori, Yasuhide Morioka, Masahiko Soga, Masashi DeguchiAbstract:Abstract The discovery of novel CB2 ligands based on the 3-carbamoyl-2-pyridone derivatives by adjusting the size of side chain at 1-, 5- and 6-position is reported. The structure–activity relationship around this template lead to the identification of S-777469 as a selective CB2 receptor agonist, which exhibited the significant inhibition of scratching induced by Compound 48/80 at 1.0 mg/kg po and 10 mg/kg po (55% and 61%, respectively).
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discovery of s 444823 a potent cb1 cb2 dual agonist as an Antipruritic Agent
Bioorganic & Medicinal Chemistry Letters, 2012Co-Authors: Masahide Odan, Yoshiharu Hiramatsu, Masanao Inagaki, Hiroshi Hashizume, Yasuhiko Fujii, Susumu Mitsumori, Natsuki Ishizuka, Yasuhide Morioka, Masahiko Soga, Masashi DeguchiAbstract:Abstract The optimization of a series of 3-carbamoyl 2-pyridone derivatives as CB agonists is reported. These efforts resulted in the discovery of 3-(2-(1-(cyclohexylmethyl)-2-oxo-1,2,5,6,7,8,9,10-octahydrocycloocta[b]pyridine-3-carboxamido)thiazol-4-yl)propanoic acid ( 21 ), a potent dual CB1/CB2 agonist without CNS side effects induced by CB1 receptor activation. It exhibited strong inhibition of scratching as a 1.0% acetone solution in the pruritic model.
Susumu Mitsumori - One of the best experts on this subject based on the ideXlab platform.
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discovery of s 777469 an orally available cb2 agonist as an Antipruritic Agent
Bioorganic & Medicinal Chemistry Letters, 2012Co-Authors: Masahide Odan, Natsuki Ishizuka, Yoshiharu Hiramatsu, Masanao Inagaki, Hiroshi Hashizume, Yasuhiko Fujii, Susumu Mitsumori, Yasuhide Morioka, Masahiko Soga, Masashi DeguchiAbstract:Abstract The discovery of novel CB2 ligands based on the 3-carbamoyl-2-pyridone derivatives by adjusting the size of side chain at 1-, 5- and 6-position is reported. The structure–activity relationship around this template lead to the identification of S-777469 as a selective CB2 receptor agonist, which exhibited the significant inhibition of scratching induced by Compound 48/80 at 1.0 mg/kg po and 10 mg/kg po (55% and 61%, respectively).
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discovery of s 444823 a potent cb1 cb2 dual agonist as an Antipruritic Agent
Bioorganic & Medicinal Chemistry Letters, 2012Co-Authors: Masahide Odan, Yoshiharu Hiramatsu, Masanao Inagaki, Hiroshi Hashizume, Yasuhiko Fujii, Susumu Mitsumori, Natsuki Ishizuka, Yasuhide Morioka, Masahiko Soga, Masashi DeguchiAbstract:Abstract The optimization of a series of 3-carbamoyl 2-pyridone derivatives as CB agonists is reported. These efforts resulted in the discovery of 3-(2-(1-(cyclohexylmethyl)-2-oxo-1,2,5,6,7,8,9,10-octahydrocycloocta[b]pyridine-3-carboxamido)thiazol-4-yl)propanoic acid ( 21 ), a potent dual CB1/CB2 agonist without CNS side effects induced by CB1 receptor activation. It exhibited strong inhibition of scratching as a 1.0% acetone solution in the pruritic model.
Yasuhiko Fujii - One of the best experts on this subject based on the ideXlab platform.
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discovery of s 777469 an orally available cb2 agonist as an Antipruritic Agent
Bioorganic & Medicinal Chemistry Letters, 2012Co-Authors: Masahide Odan, Natsuki Ishizuka, Yoshiharu Hiramatsu, Masanao Inagaki, Hiroshi Hashizume, Yasuhiko Fujii, Susumu Mitsumori, Yasuhide Morioka, Masahiko Soga, Masashi DeguchiAbstract:Abstract The discovery of novel CB2 ligands based on the 3-carbamoyl-2-pyridone derivatives by adjusting the size of side chain at 1-, 5- and 6-position is reported. The structure–activity relationship around this template lead to the identification of S-777469 as a selective CB2 receptor agonist, which exhibited the significant inhibition of scratching induced by Compound 48/80 at 1.0 mg/kg po and 10 mg/kg po (55% and 61%, respectively).
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discovery of s 444823 a potent cb1 cb2 dual agonist as an Antipruritic Agent
Bioorganic & Medicinal Chemistry Letters, 2012Co-Authors: Masahide Odan, Yoshiharu Hiramatsu, Masanao Inagaki, Hiroshi Hashizume, Yasuhiko Fujii, Susumu Mitsumori, Natsuki Ishizuka, Yasuhide Morioka, Masahiko Soga, Masashi DeguchiAbstract:Abstract The optimization of a series of 3-carbamoyl 2-pyridone derivatives as CB agonists is reported. These efforts resulted in the discovery of 3-(2-(1-(cyclohexylmethyl)-2-oxo-1,2,5,6,7,8,9,10-octahydrocycloocta[b]pyridine-3-carboxamido)thiazol-4-yl)propanoic acid ( 21 ), a potent dual CB1/CB2 agonist without CNS side effects induced by CB1 receptor activation. It exhibited strong inhibition of scratching as a 1.0% acetone solution in the pruritic model.