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Synthesis and Antinociceptive activity of Newly Modified Amine analogs of Phencyclidine in Mice


Maryam Shokrollahi, Marjaneh Samadizadeh, Mohsen Khalili, Seyed Ali Sobhanian and Abbas Ahmadi*  


Background: Phencyclidine (PCP, I) and its substituted analogs are significant and broadly abused psychotomimetic drugs that affect the central nervous system. They show many pharmacological properties due to the presence of specific receptors in the brain.

Aim and Objective: Methyl group, despite strong electron-donating and characters of dipole moments, were placed on various positions of phenyl and amine moieties of Phencyclidine along with the substitution of benzylamine, piperazine, and aniline derivatives in place of piperidine ring of Phencyclidine to create novel compounds of the core with analgesic properties.

Material and methods: For evaluation of the Analgesic activities of newly synthesized compounds, they were screened by tests of tail immersion (thermal) and formalin (chemical) pains. The obtained data with the control and PCP groups were compared too.

Results: The outcomes indicated that some new compounds have more antinociceptive effects than PCP in tail immersion and formalin tests. In the tail immersion test, the methyl piperazine analog (III) shows more efficacy than others. In the formalin test, none of the compounds are as effective as phencyclidine at the earliest time-point, but compounds IV and V do show more effective during the second stage of formalin pain.

Conclusion: It can be concluded that the methyl-piperazine analog of phencyclidine was the best candidate to decrease acute thermal and benzylamine derivatives were suitable candidates to reduce chemical pains.


Synthesis, Antinociceptive activity, Benzylamine, Piperazineand Aniline Phencyclidine's derivatives, Central Nervous System, Tail Immersion and formalin tests


Department of Chemistry, Faculty of Science, Centeral Tehran Branch, Islamic Azad University, Karaj, Department of Chemistry, Faculty of Science, Centeral Tehran Branch, Islamic Azad University, Karaj, Neurophysiology Research Center, Shahed University, Tehran, Department of Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Tehran Medical Sciences, Islamic Azad University, Tehran, Department of Chemistry, Faculty of Science, Karaj Branch, Islamic Azad University, Karaj

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