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| Routes of administration | IV |
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| Formula | C26H26N2O3 |
| Molar mass | 414.505 g·mol−1 |
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Naltrindole is a highly potent, highly selectivedelta opioid receptorantagonist used in biomedical research. In May 2012 a paper was published inNature with the structure of naltrindole in complex with the mouse δ-opioid G-protein coupled receptor, solved by X-ray crystallography.[1]
Sincepeptide compounds are unable to cross theblood–brain barrier, researchers developed naltrindole to be a non-peptide antagonist analog of thedelta-preferring endogenous opiateenkephalin. Enkephalin contains anaromaticphenyl group on itsPhe4 residue, which was hypothesized to be the "address" sequence responsible for the opiate's delta opioid receptor affinity.[2] Thus, attachment of a phenyl-containingindole molecule to the C-ring ofnaltrexone'smorphinan base successfully produced a drug with the high receptor affinity of naltrexone, but which binds almost exclusively to the delta opioid receptor.[3]
