“Taranabant”的意思、由来-开放百科全书

In October 2008, Merck has stopped its phase III clinical trials with the drugs due to high level of central side effects, mainly depression and anxiety.^[3]^[4]^[5]^[6]

References

1. ^Armstrong HE, Galka A, Lin LS, Lanza TJ Jr, Jewell JP, Shah SK, et al. "Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists." Bioorganic & Medicinal Chemistry Letters. 2007 Apr 15;17(8):2184-7. {{PMID|17293109}}. {{doi|10.1016/j.bmcl.2007.01.087}}
2. ^Fong TM, Guan XM, Marsh DJ, Shen CP, Stribling DS, Rosko KM, et al. "Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents." Journal of Pharmacology and Experimental Therapeutics. 2007 Jun;321(3):1013-22. {{PMID|17327489}}. {{doi|10.1124/jpet.106.118737}}
3. ^{{cite web |url=http://www.merck.com/newsroom/press_releases/research_and_development/2008_1002.html |title=Press release by Merck |work= |accessdate=October 2008}}
4. ^{{cite journal |vauthors=Aronne LJ, Tonstad S, Moreno M, Gantz I, Erondu N, Suryawanshi S, Molony C, Sieberts S, Nayee J, Meehan AG, Shapiro D, Heymsfield SB, Kaufman KD, Amatruda JM |title=A clinical trial assessing the safety and efficacy of taranabant, a CB1R inverse agonist, in obese and overweight patients: a high-dose study |journal=International Journal of Obesity |volume=34 |issue=5 |pages=919–35 |date=May 2010 |pmid=20157323 |doi=10.1038/ijo.2010.21 |url=}}
5. ^{{cite journal |vauthors=Kipnes MS, Hollander P, Fujioka K, Gantz I, Seck T, Erondu N, Shentu Y, Lu K, Suryawanshi S, Chou M, Johnson-Levonas AO, Heymsfield SB, Shapiro D, Kaufman KD, Amatruda JM |title=A one-year study to assess the safety and efficacy of the CB1R inverse agonist taranabant in overweight and obese patients with type 2 diabetes |journal=Diabetes, Obesity & Metabolism |volume=12 |issue=6 |pages=517–31 |date=June 2010 |pmid=20518807 |doi=10.1111/j.1463-1326.2009.01188.x |url=}}
6. ^{{cite journal |vauthors=Proietto J, Rissanen A, Harp JB, Erondu N, Yu Q, Suryawanshi S, Jones ME, Johnson-Levonas AO, Heymsfield SB, Kaufman KD, Amatruda JM |title=A clinical trial assessing the safety and efficacy of the CB1R inverse agonist taranabant in obese and overweight patients: low-dose study |journal=International Journal of Obesity |volume=34 |issue=8 |pages=1243–54 |date=August 2010 |pmid=20212496 |doi=10.1038/ijo.2010.38 |url=}}

词条	Taranabant
释义	See also References {{Drugbox \| Watchedfields = changed \| verifiedrevid = 448081332 \| IUPAC_name = N-[(2S,3S)-4-(4-chlorophenyl)-3-(3-cyanophenyl)-2-butanyl]-2-methyl-2-{[5-(trifluoromethyl)-2-pyridinyl]oxy}propanamide \| image = Taranabant.png \| alt = Skeletal formula of taranabant \| width = 250 \| image2 = Taranabant 3D spacefill.png \| alt2 = Space-filling model of the taranabant molecule \| tradename = \| pregnancy_AU = \| pregnancy_US = \| pregnancy_category = \| legal_AU = \| legal_CA = \| legal_UK = \| legal_US = \| legal_status = Investigational (failed) \| routes_of_administration = Oral \| bioavailability = \| protein_bound = \| metabolism = \| elimination_half-life = \| excretion = \| CAS_number_Ref = {{cascite\|correct\|??}} \| CAS_number = 701977-09-5 \| ATC_prefix = A08 \| ATC_suffix = AX \| PubChem = 11226090 \| DrugBank_Ref = {{drugbankcite\|correct\|drugbank}} \| DrugBank = \| UNII_Ref = {{fdacite\|correct\|FDA}} \| UNII = X9U622S114 \| ChemSpiderID = 9401143 \| chemical_formula = \| C=27 \| H=25 \| Cl=1 \| F=3 \| N=3 \| O=2 \| molecular_weight = 515.95 g/mol \| smiles = C[C@@H]([C@@H](CC1=CC=C(C=C1)Cl)C2=CC=CC(=C2)C#N)NC(=O)C(C)(C)OC3=NC=C(C=C3)C(F)(F)F \| StdInChI = 1S/C27H25ClF3N3O2/c1-17(34-25(35)26(2,3)36-24-12-9-21(16-33-24)27(29,30)31)23(14-18-7-10-22(28)11-8-18)20-6-4-5-19(13-20)15-32/h4-13,16-17,23H,14H2,1-3H3,(H,34,35)/t17-,23+/m0/s1 \| StdInChIKey = QLYKJCMUNUWAGO-GAJHUEQPSA-N }}Taranabant (codenamed MK-0364) is a cannabinoid receptor type 1 inverse agonist that was investigated as a potential treatment for obesity due to its anorectic effects.^[1]^[2] It was discovered by Merck & Co. In October 2008, Merck has stopped its phase III clinical trials with the drugs due to high level of central side effects, mainly depression and anxiety.^[3]^[4]^[5]^[6] See also Cannabinoid receptor antagonist References 1. ^Armstrong HE, Galka A, Lin LS, Lanza TJ Jr, Jewell JP, Shah SK, et al. "Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists." Bioorganic & Medicinal Chemistry Letters. 2007 Apr 15;17(8):2184-7. {{PMID\|17293109}}. {{doi\|10.1016/j.bmcl.2007.01.087}} 2. ^Fong TM, Guan XM, Marsh DJ, Shen CP, Stribling DS, Rosko KM, et al. "Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents." Journal of Pharmacology and Experimental Therapeutics. 2007 Jun;321(3):1013-22. {{PMID\|17327489}}. {{doi\|10.1124/jpet.106.118737}} 3. ^{{cite web \|url=http://www.merck.com/newsroom/press_releases/research_and_development/2008_1002.html \|title=Press release by Merck \|work= \|accessdate=October 2008}} 4. ^{{cite journal \|vauthors=Aronne LJ, Tonstad S, Moreno M, Gantz I, Erondu N, Suryawanshi S, Molony C, Sieberts S, Nayee J, Meehan AG, Shapiro D, Heymsfield SB, Kaufman KD, Amatruda JM \|title=A clinical trial assessing the safety and efficacy of taranabant, a CB1R inverse agonist, in obese and overweight patients: a high-dose study \|journal=International Journal of Obesity \|volume=34 \|issue=5 \|pages=919–35 \|date=May 2010 \|pmid=20157323 \|doi=10.1038/ijo.2010.21 \|url=}} 5. ^{{cite journal \|vauthors=Kipnes MS, Hollander P, Fujioka K, Gantz I, Seck T, Erondu N, Shentu Y, Lu K, Suryawanshi S, Chou M, Johnson-Levonas AO, Heymsfield SB, Shapiro D, Kaufman KD, Amatruda JM \|title=A one-year study to assess the safety and efficacy of the CB1R inverse agonist taranabant in overweight and obese patients with type 2 diabetes \|journal=Diabetes, Obesity & Metabolism \|volume=12 \|issue=6 \|pages=517–31 \|date=June 2010 \|pmid=20518807 \|doi=10.1111/j.1463-1326.2009.01188.x \|url=}} 6. ^{{cite journal \|vauthors=Proietto J, Rissanen A, Harp JB, Erondu N, Yu Q, Suryawanshi S, Jones ME, Johnson-Levonas AO, Heymsfield SB, Kaufman KD, Amatruda JM \|title=A clinical trial assessing the safety and efficacy of the CB1R inverse agonist taranabant in obese and overweight patients: low-dose study \|journal=International Journal of Obesity \|volume=34 \|issue=8 \|pages=1243–54 \|date=August 2010 \|pmid=20212496 \|doi=10.1038/ijo.2010.38 \|url=}} {{Anorectics}}{{Cannabinoids}}{{Cannabinoidergics}}{{cannabinoid-stub}} 8 : Anorectics\|Cannabinoids\|CB1 receptor antagonists\|Pyridines\|Nitriles\|Chloroarenes\|Trifluoromethyl compounds\|Carboxamides
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See also

References