Clocinnamox

Clocinnamox.svg

Clocinnamox is a synthetic opioid antagonist that is used in scientific research to study the opioid receptor system. It is particularly known for its ability to selectively and irreversibly block the mu-opioid receptor (MOR), which is one of the three main types of opioid receptors, the others being the delta-opioid receptor (DOR) and the kappa-opioid receptor (KOR).

Chemical Structure and Properties

Clocinnamox belongs to the class of 4-phenylpiperidine derivatives. Its chemical structure is characterized by the presence of a phenyl ring and a piperidine ring, which are essential for its binding affinity to the mu-opioid receptor. The irreversible binding of clocinnamox to the MOR is due to its ability to form a covalent bond with the receptor, leading to long-lasting antagonistic effects.

Mechanism of Action

Clocinnamox acts by binding irreversibly to the mu-opioid receptor, thereby preventing the activation of the receptor by endogenous opioid peptides such as endorphins and enkephalins, as well as exogenous opioid drugs like morphine and heroin. This irreversible binding results in a prolonged blockade of the receptor, making clocinnamox a valuable tool in opioid research for studying the long-term effects of opioid receptor inhibition.

Research Applications

Clocinnamox is primarily used in preclinical research to investigate the role of the mu-opioid receptor in various physiological and pathological processes. It has been employed in studies examining pain management, addiction, and tolerance to opioid drugs. By irreversibly blocking the mu-opioid receptor, researchers can better understand the receptor's function and its involvement in opioid-related behaviors.

Pharmacokinetics

The pharmacokinetics of clocinnamox involve its absorption, distribution, metabolism, and excretion. Due to its irreversible binding to the mu-opioid receptor, the duration of its antagonistic effects is significantly longer compared to reversible opioid antagonists like naloxone and naltrexone. This makes clocinnamox particularly useful for long-term studies on opioid receptor function.

Safety and Toxicity

As with other opioid antagonists, the safety and toxicity profile of clocinnamox must be carefully considered in research settings. While it is not used clinically, its effects on the opioid system can provide insights into the potential risks and benefits of opioid receptor modulation.

See Also

• Opioid receptor
• Mu-opioid receptor
• Delta-opioid receptor
• Kappa-opioid receptor
• Opioid antagonist
• Naloxone
• Naltrexone
• Endorphins
• Enkephalins