ArticleNaunyn-Schmiedeberg's archives of pharmacology2013
The in vitro pharmacological profile of TD-1211, a neutral opioid receptor antagonist.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 12 citations in OpenAlex.
- Phenol (bio)isosteres in drug design and development.Archiv der Pharmazie · 2025Review
- Ligand-Free Signaling of G-Protein-Coupled Receptors: Relevance to μ Opioid Receptors in Analgesia and Addiction.Molecules (Basel, Switzerland) · 2022Review
- Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.ACS medicinal chemistry letters · 2019Article
- Peripherally Acting μ-Opioid Receptor Antagonists for the Treatment of Opioid-Related Side Effects: Mechanism of Action and Clinical Implications.Journal of pharmacy practice · 2018Review
- New Options in Constipation Management.Current oncology reports · 2015Review
- Novel therapeutic agents in neurogastroenterology: advances in the past year.Neurogastroenterology and motility · 2014Review
- The in vivo pharmacodynamics of the novel opioid receptor antagonist, TD-1211, in models of opioid-induced gastrointestinal and CNS activity.Naunyn-Schmiedeberg's archives of pharmacology · 2013Article
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
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 recombinant μ and δ, and guinea pig κ receptors expressed in CHO-K1 cells (pK d = 9.7, 8.6, and 9.9, respectively). The in vitro receptor selectivity of TD-1211 (μ ≈ κ > δ) is similar to that for the peripherally-selective opioid receptor antagonist methylnaltrexone, but contrasts with the μ selectivity of alvimopan. Functionally, TD-1211 behaved as an antagonist at all three receptor types in both recombinant expression systems (pK b = 9.6, 8.8 and 9.5, at μ, δ, and κ, respectively) and rodent native tissue preparations (μ and κ pA2s = 10.1 and 8.8, respectively (guinea pig ileum), and δ pK b = 8.4 (hamster vas deferens)). TD-1211 displayed a high degree of selectivity for opioid receptors over a broad panel of cellular targets. These in vitro data justified investigation of the preclinical in vivo activity of TD-1211 (Armstrong et al., Naunyn-Schmiedeberg's Arch Pharm, 2013).
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.