Synthesis and Antinociception Activities of Some Novel Derivatives of Phencyclidine with Substituted Aminobenzothiazoles.
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 &amp;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 &amp; phencyclidine animal groups.


CONCLUSIONS
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.
Applied Chemistry, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran, No 99, Yakhchal, Gholhak, Shariati, Tehran, Iran.
Abbas
A
Ahmadi
Mohsen
M
Khalili
Behrooz
B
Mirza
Mojtaba
M
Mohammadi-Diz
Farnaz
F
Azami-Lorestani
Parisa
P
Ghaderi
Babak
B
Nahri-Niknafs
D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D000818:Animals; D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D006801:Humans; D015394:Molecular Structure; D010146:Pain / Q000188:drug therapy*; D010622:Phencyclidine / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*
D000700:Analgesics; D052160:Benzothiazoles; C523775:aminobenzothiazole compound; D010622:Phencyclidine