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o-PCP (2-Keto-Phencyclidine): A Potent Arylcyclohexylamine Dissociative

Overview

o-PCP, also known as 2-keto-phencyclidine, is a synthetic arylcyclohexylamine derivative structurally related to phencyclidine (PCP). It belongs to the class of dissociative anesthetics, acting primarily as an N-methyl-D-aspartate (NMDA) receptor antagonist. This mechanism disrupts excitatory neurotransmission, leading to the characteristic dissociative effects observed with compounds in this class.

Chemical Properties

• IUPAC名： 1-[1-(2-Ketocyclohexyl)phenyl]piperidine
• 分子式： C17H23NO
• 分子量： Approximately 257.37 g/mol
• Chemical Class: Arylcyclohexylamine
• Structural Features: Incorporates a ketone group at the 2-position of the cyclohexyl ring, distinguishing it from PCP.

薬力学

o-PCP functions as a non-competitive antagonist at the NMDA receptor, inhibiting the action of glutamate, the primary excitatory neurotransmitter in the central nervous system. This blockade leads to a decrease in neuronal excitability, resulting in anesthetic and dissociative effects. The presence of the ketone group may influence its binding affinity and pharmacological profile compared to PCP.

薬物動態学

While specific pharmacokinetic data for o-PCP are limited, analogs in the arylcyclohexylamine class typically exhibit:

• Absorption: Rapid onset of action when administered via inhalation or intravenous routes.
• Distribution: High lipid solubility allows for extensive distribution into the central nervous system.
• Metabolism: Primarily hepatic, involving cytochrome P450 enzymes.
• Elimination: Renal excretion of metabolites.

用法・用量

Due to the lack of clinical data, standardized dosing guidelines for o-PCP are not established. In research settings, dosing must be approached with caution, starting with minimal amounts to assess potency and effect. It is imperative to note that o-PCP is not approved for human consumption and should only be handled in controlled laboratory environments.

効果

• Desired Effects:
  • Dissociation from environment and self
  • Analgesia
  • Altered sensory perception
  • Euphoria
• Adverse Effects:
  • 混乱
  • Agitation
  • Hallucinations
  • Tachycardia
  • 高血圧
  • Potential neurotoxicity with high doses or prolonged exposure

Safety and Harm Reduction

Given its potency and the limited understanding of its full pharmacological profile, o-PCP poses significant risks:

• Neurotoxicity: Potential for neuronal damage with excessive or prolonged use.
• Psychological Effects: Risk of inducing psychosis, especially in individuals predisposed to mental health disorders.
• Physical Risks: Impaired motor function increases the likelihood of accidents.
• Dependence: Potential for abuse and development of tolerance.

Legal Status

The legal classification of o-PCP varies by jurisdiction. In many regions, it may be considered a controlled substance analog, subject to regulation under analog laws. Researchers must ensure compliance with local regulations when handling this compound.

結論

o-PCP is a potent dissociative agent within the arylcyclohexylamine class, exhibiting significant NMDA receptor antagonism. Its structural similarity to PCP suggests comparable effects, though the presence of the ketone group may alter its pharmacological profile. Due to its potency and potential risks, o-PCP should be handled with extreme caution and is intended solely for research purposes in controlled settings.

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