7-Benzylidenenaltrexone

From WikiMD's medical encyclopedia

7-Benzylidenenaltrexone (BNTX) is a selective opioid receptor antagonist, specifically targeting the delta opioid receptor (DOR). It is a derivative of naltrexone, a well-known opioid antagonist used in the treatment of opioid addiction and alcohol dependence.

Pharmacology

7-Benzylidenenaltrexone acts by binding to the delta opioid receptors in the central nervous system, thereby inhibiting the effects of endogenous opioids such as enkephalins. Unlike non-selective opioid antagonists, BNTX does not significantly affect the mu opioid receptor (MOR) or the kappa opioid receptor (KOR), making it a valuable tool in research to study the specific roles of delta receptors in pain modulation, mood regulation, and other physiological processes.

Research Applications

BNTX is primarily used in scientific research to explore the function of delta opioid receptors. Studies have shown that delta receptors are involved in modulating analgesia, mood, and neuroprotection. By selectively blocking these receptors, researchers can better understand their role in various conditions, including chronic pain, depression, and neurodegenerative diseases.

Chemical Structure

The chemical structure of 7-Benzylidenenaltrexone is characterized by the presence of a benzylidene group attached to the naltrexone backbone. This modification enhances its selectivity for the delta opioid receptor. The compound has a molecular formula of C26H25NO4 and a molecular weight of 415.48 g/mol.

Synthesis

The synthesis of 7-Benzylidenenaltrexone involves the chemical modification of naltrexone. The process typically includes the introduction of a benzylidene moiety at the 7-position of the naltrexone molecule. This synthetic route is crucial for producing the compound in sufficient quantities for research purposes.

Potential Therapeutic Uses

While primarily a research tool, the selective antagonism of delta opioid receptors by BNTX suggests potential therapeutic applications. These may include the treatment of conditions where delta receptor activity is implicated, such as certain types of pain and mood disorders. However, further research is needed to explore these possibilities.

Safety and Toxicology

As with many research chemicals, the safety profile of 7-Benzylidenenaltrexone is not fully established. It is used under controlled laboratory conditions, and its effects in humans are not well-documented. Researchers must exercise caution and adhere to safety protocols when handling this compound.

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Contributors: Prab R. Tumpati, MD