Naltrindole

Naltrindole is a highly potent, highly selective delta opioid receptor antagonist used in biomedical research.

Since peptide compounds are unable to cross the blood brain barrier, researchers developed naltrindole to be a non-peptide antagonist analog of the delta-preferring endogenous opiate enkephalin. Enkephalin contains an aromatic phenyl group on its Phe⁴ residue, which was hypothesized to be the “address” sequence responsible for the opiate’s delta opioid receptor affinity^[1]. Thus, attachment of a phenyl-containing indole molecule to the C-ring of naltrexone‘s morphinan base successfully produced a drug with the high receptor affinity of naltrexone, but which binds almost exclusively to the delta opioid receptor^[2].

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