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The in vitro pharmacology of the peripherally restricted opioid receptor antagonists, alvimopan, ADL 08-0011 and methylnaltrexone.
Beattie DT, Cheruvu M, Mai N, O'Keefe M, Johnson-Rabidoux S, Peterson C, Kaufman E, Vickery R. Beattie DT, et al. Naunyn Schmiedebergs Arch Pharmacol. 2007 May;375(3):205-20. doi: 10.1007/s00210-007-0146-x. Epub 2007 Mar 6. Naunyn Schmiedebergs Arch Pharmacol. 2007. PMID: 17340127
Alvimopan and ADL 08-0011 had higher binding affinity than methylnaltrexone at human mu opioid receptors (pK (i) values of 9.6, 9.6, and 8.0, respectively). ...In tissue from morphine-dependent animals, alvimopan and ADL 08-0011 increased …
Alvimopan and ADL 08-0011 had higher binding affinity than methylnaltrexone at human mu opioid receptors (pK (i) values …
The in vivo pharmacodynamics of the novel opioid receptor antagonist, TD-1211, in models of opioid-induced gastrointestinal and CNS activity.
Armstrong SR, Campbell CB, Richardson CL, Vickery RG, Tsuruda PR, Long DD, Hegde SS, Beattie DT. Armstrong SR, et al. Naunyn Schmiedebergs Arch Pharmacol. 2013 Jun;386(6):471-8. doi: 10.1007/s00210-013-0844-5. Epub 2013 Mar 13. Naunyn Schmiedebergs Arch Pharmacol. 2013. PMID: 23512167
Oral administration of TD-1211, naltrexone, and ADL 08-0011 reversed loperamide-induced inhibition of gastric emptying and castor oil-induced diarrhea in rats and nonproductive GI circular smooth muscle contractility in dogs. Alvimopan was only efficacious in …
Oral administration of TD-1211, naltrexone, and ADL 08-0011 reversed loperamide-induced inhibition of gastric emptying …