O-1376

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O-1376

O-1376 is a synthetic opioid analgesic that has been studied for its potential use in pain management. It is part of a class of drugs known as opioids, which are substances that act on opioid receptors to produce morphine-like effects. O-1376 is notable for its potency and its potential applications in both clinical and research settings.

Chemical Structure and Properties

O-1376 is chemically related to other opioids, sharing a core structure that interacts with the central nervous system. The molecular formula of O-1376 is C22H28N2O2, and it has a molecular weight of 352.47 g/mol. The compound is typically synthesized in a laboratory setting, using a series of chemical reactions that build upon simpler organic molecules.

Pharmacology

O-1376 functions primarily as a mu-opioid receptor agonist. This means that it binds to and activates the mu-opioid receptors in the brain and spinal cord, which are responsible for the analgesic (pain-relieving) effects of opioids. The activation of these receptors leads to a decrease in the perception of pain, as well as a potential for euphoria, which can contribute to the risk of addiction.

Mechanism of Action

The mechanism of action of O-1376 involves the inhibition of neurotransmitter release in the central nervous system. By binding to the mu-opioid receptors, O-1376 reduces the release of substance P and other neurotransmitters involved in the transmission of pain signals. This results in an increased pain threshold and a reduction in the sensation of pain.

Pharmacokinetics

The pharmacokinetics of O-1376, including its absorption, distribution, metabolism, and excretion, are critical for understanding its effects and potential therapeutic uses. O-1376 is typically administered via intravenous injection, allowing for rapid onset of action. It is metabolized in the liver and excreted primarily through the kidneys.

Clinical Applications

While O-1376 has shown promise in preclinical studies, its use in clinical settings is limited due to concerns about safety and the potential for abuse. Research is ongoing to determine the appropriate dosing regimens and to develop formulations that minimize the risk of addiction.

Safety and Side Effects

As with other opioids, the use of O-1376 is associated with a range of side effects. Common side effects include nausea, vomiting, constipation, and drowsiness. More serious risks include respiratory depression, which can be life-threatening, and the potential for addiction and abuse.

Regulatory Status

O-1376 is not currently approved for medical use by major regulatory agencies such as the FDA or EMA. It is classified as a research chemical, and its use is restricted to scientific studies and laboratory research.

Research and Development

Ongoing research into O-1376 focuses on its potential as a pain management option, particularly in cases where traditional opioids are ineffective or contraindicated. Studies are also exploring its pharmacological profile and the development of safer analogs with reduced abuse potential.

Also see

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Contributors: Prab R. Tumpati, MD