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Naltrindole
Naltrindole is a highly potent, highly selective delta opioid receptor antagonist used in biomedical research. Product highlightDrug DesignSince 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]. References
Categories: Opioids | Opioid antagonists |
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This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Naltrindole". A list of authors is available in Wikipedia. |