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'''Taranabant''' (codenamed MK-0364) is a [[cannabinoid receptor type 1]] [[inverse agonist]] being investigated as a potential treatment for [[obesity]] due to its [[anorectic]] effects.<ref>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}}</ref><ref>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}}</ref> It was discovered by [[Merck & Co.]]
'''Taranabant''' (codenamed MK-0364) is a [[cannabinoid receptor type 1]] [[inverse agonist]] being investigated as a potential treatment for [[obesity]] due to its [[anorectic]] effects.<ref>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}}</ref><ref>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}}</ref> It was discovered by [[Merck & Co.]]


In October 2008, Merck has stopped its [[Clinical_trials#Phase_III|phase III]] [[clinical trials]] with the drugs due to high level of central side effects, mainly depression and anxiety.<ref name="urlMerck News Item">{{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}}</ref><ref name="pmid20157323">{{cite journal |author=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 (2005) |volume=34 |issue=5 |pages=919–35 |year=2010 |month=May |pmid=20157323 |doi=10.1038/ijo.2010.21 |url=}}</ref><ref name="pmid20518807">{{cite journal |author=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 |year=2010 |month=June |pmid=20518807 |doi=10.1111/j.1463-1326.2009.01188.x |url=}}</ref><ref name="pmid20212496">{{cite journal |author=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 (2005) |volume=34 |issue=8 |pages=1243–54 |year=2010 |month=August |pmid=20212496 |doi=10.1038/ijo.2010.38 |url=}}</ref>
In October 2008, Merck has stopped its [[Clinical_trials#Phase_III|phase III]] [[clinical trials]] with the drugs due to high level of [[central nervous system|central]] side effects, mainly [[depression]] and [[anxiety]].<ref name="urlMerck News Item">{{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}}</ref><ref name="pmid20157323">{{cite journal |author=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 (2005) |volume=34 |issue=5 |pages=919–35 |year=2010 |month=May |pmid=20157323 |doi=10.1038/ijo.2010.21 |url=}}</ref><ref name="pmid20518807">{{cite journal |author=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 |year=2010 |month=June |pmid=20518807 |doi=10.1111/j.1463-1326.2009.01188.x |url=}}</ref><ref name="pmid20212496">{{cite journal |author=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 (2005) |volume=34 |issue=8 |pages=1243–54 |year=2010 |month=August |pmid=20212496 |doi=10.1038/ijo.2010.38 |url=}}</ref>



== See also ==
== See also ==

Revision as of 02:05, 24 December 2010

Taranabant
Clinical data
Routes of
administration		Oral
ATC code
Identifiers
  • N-[(1S,2S)-3-(4-Chlorophenyl)-2-

    (3-cyanophenyl)-1-methylpropyl]-2-methyl-2-

    ((5-(trifluoromethyl)pyridin-2-yl)oxy)propanamide
CAS Number
PubChem CID
CompTox Dashboard (EPA)
ECHA InfoCard100.207.983 Edit this at Wikidata
Chemical and physical data
FormulaC27H25ClF3N3O2
Molar mass515.95 g·mol−1

Taranabant (codenamed MK-0364) is a cannabinoid receptor type 1 inverse agonist being 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

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. ^ "Press release by Merck". Retrieved October 2008. {{cite web}}: Check date values in: |accessdate= (help)
  4. ^ 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 (2010). "A clinical trial assessing the safety and efficacy of taranabant, a CB1R inverse agonist, in obese and overweight patients: a high-dose study". International Journal of Obesity (2005). 34 (5): 919–35. doi:10.1038/ijo.2010.21. PMID 20157323. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  5. ^ 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 (2010). "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". Diabetes, Obesity & Metabolism. 12 (6): 517–31. doi:10.1111/j.1463-1326.2009.01188.x. PMID 20518807. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  6. ^ Proietto J, Rissanen A, Harp JB, Erondu N, Yu Q, Suryawanshi S, Jones ME, Johnson-Levonas AO, Heymsfield SB, Kaufman KD, Amatruda JM (2010). "A clinical trial assessing the safety and efficacy of the CB1R inverse agonist taranabant in obese and overweight patients: low-dose study". International Journal of Obesity (2005). 34 (8): 1243–54. doi:10.1038/ijo.2010.38. PMID 20212496. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)


source: https://en.wikipedia.org/w/index.php?title=Taranabant&diff=prev&oldid=403967393

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