949904-48-7
Chemical Structure
Axelopran
Synonym(s): TD-1211
- CAS No.: 949904-48-7
- Formula:C26H39N3O4
- Molecular Weight:457.61
IUPAC Name: 3-((1R,3S,5S)-8-(2-((S)-N-(cyclohexylmethyl)-2,3-dihydroxypropanamido)ethyl)-8-azabicyclo[3.2.1]octan-3-yl)benzamide
InChIKey: ATLYLVPZNWDJBW-KIHHCIJBSA-N
SMILES: O=C([C@@H](O)CO)N(CC1CCCCC1)CCN2[C@H]3C[C@H](C4=CC(C(N)=O)=CC=C4)C[C@@H]2CC3
Biological Activity: Axelopran (TD-1211) is an orally active opioid receptor antagonist. Axelopran binds to human μ-, δ-, and κ-opioid receptors with pKi values of 9.8, 8.8, and 9.9, respectively. Axelopran (sulfate) blocks μ-opioid receptor agonist signaling, reverses opioid-induced gastrointestinal inhibition, and inhibits agonist-induced opioid receptor G protein activation. Axelopran can be used for research on opioid-induced constipation[1][2].
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Axelopran | Axelopran (TD-1211) is an orally active opioid receptor antagonist. Axelopran binds to human μ-, δ-, and κ-opioid receptors with pKi values of 9.8, 8.8, and 9.9, respectively. Axelopran (sulfate) blocks μ-opioid receptor agonist signaling, reverses opioid-induced gastrointestinal inhibition, and inhibits agonist-induced opioid receptor G protein activation. Axelopran can be used for research on opioid-induced constipation. | |||||||||||||||||||||
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References
- [1]. Long DD, et al. Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist. ACS Med Chem Lett. 2019 Nov 26;10(12):1641-1647.
- [2]. Armstrong SR, et al. 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. 2013 Jun;386(6):471-8.
