Abstract
Background: Phencyclidine (PCP) as well as the analogues has indicated several pharmacological behaviors like analgesic, anticonvulsant, antianxiety, antidepressant depending on the dose and species examined. They interact with some neurotransmitter systems in the central nervous system like particular affinity for PCP sites in NMDA receptors or dopamine uptake blocking or both.
Objective: Due to analgesic properties of aminobenzothiazoles family, piperidine ring of PCP was replaced with electron-donating and electron-withdrawing substituted aminobenzothiazoles (1-4) for obtaining new analogues (II-V) with more analgesic activities.
Methods: Synthesis of new compounds (II-V) and measuring the acute and chronic pain properties of them were carried out through applying tail immersion &formalin tests on mice and the outcomes compared with control & PCP groups at dosage of 10 mg/kg.
Results: III & V with substituted methoxy and methyl-aminobenzothiazoles indicated better activity to lessen acute and chronic (thermal and chemical) pains compared with unsubstituted & phencyclidine animal groups.
Conclusion: Methoxy and methyl-aminobenzothiazole derivatives” of phencyclidine revealed more analgesic activities compared with other groups which may concern to close affinity for DA uptake blocking as well as NMDA receptors in this family.
Keywords: Aminobenzothiazole substituted of phencyclidine, dopamine uptake blocking, NMDA receptors, tail immersion and formalin tests.
Mini-Reviews in Medicinal Chemistry
Title:Synthesis and Antinociception Activities of Some Novel Derivatives of Phencyclidine with Substituted Aminobenzothiazoles
Volume: 17 Issue: 1
Author(s): Abbas Ahmadi, Mohsen Khalili, Behrooz Mirza, Mojtaba Mohammadi-Diz, Farnaz Azami-Lorestani, Parisa Ghaderi and Babak Nahri-Niknafs
Affiliation:
Keywords: Aminobenzothiazole substituted of phencyclidine, dopamine uptake blocking, NMDA receptors, tail immersion and formalin tests.
Abstract: Background: Phencyclidine (PCP) as well as the analogues has indicated several pharmacological behaviors like analgesic, anticonvulsant, antianxiety, antidepressant depending on the dose and species examined. They interact with some neurotransmitter systems in the central nervous system like particular affinity for PCP sites in NMDA receptors or dopamine uptake blocking or both.
Objective: Due to analgesic properties of aminobenzothiazoles family, piperidine ring of PCP was replaced with electron-donating and electron-withdrawing substituted aminobenzothiazoles (1-4) for obtaining new analogues (II-V) with more analgesic activities.
Methods: Synthesis of new compounds (II-V) and measuring the acute and chronic pain properties of them were carried out through applying tail immersion &formalin tests on mice and the outcomes compared with control & PCP groups at dosage of 10 mg/kg.
Results: III & V with substituted methoxy and methyl-aminobenzothiazoles indicated better activity to lessen acute and chronic (thermal and chemical) pains compared with unsubstituted & phencyclidine animal groups.
Conclusion: Methoxy and methyl-aminobenzothiazole derivatives” of phencyclidine revealed more analgesic activities compared with other groups which may concern to close affinity for DA uptake blocking as well as NMDA receptors in this family.
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Cite this article as:
Ahmadi Abbas, Khalili Mohsen, Mirza Behrooz, Mohammadi-Diz Mojtaba, Azami-Lorestani Farnaz, Ghaderi Parisa and Nahri-Niknafs Babak, Synthesis and Antinociception Activities of Some Novel Derivatives of Phencyclidine with Substituted Aminobenzothiazoles, Mini-Reviews in Medicinal Chemistry 2017; 17 (1) . https://dx.doi.org/10.2174/1389557516666160428112532
DOI https://dx.doi.org/10.2174/1389557516666160428112532 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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