The in vitro pharmacological profile of TD-1211, a neutral opioid receptor antagonist

@article{Tsuruda2013TheIV,
  title={The in vitro pharmacological profile of TD-1211, a neutral opioid receptor antagonist},
  author={Pamela R. Tsuruda and Ross G. Vickery and Daniel D. Long and Scott R. Armstrong and David T. Beattie},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  year={2013},
  volume={386},
  pages={479-491}
}
The clinical efficacy of opioid receptor antagonists for the treatment of opioid-induced constipation (OIC) is established. Peripherally selective antagonists are intended to provide OIC symptom relief without compromising the analgesic effects of centrally penetrant opioid agonists. We describe the in vitro profile of a novel opioid receptor antagonist, TD-1211, at recombinant (human μ and δ, and guinea pig κ) and rodent native opioid receptors. TD-1211 bound with high affinity to human… 
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