Synthesis and analgesic activities of phenyl piperazinyl aralkyl ketone derivatives / 药学学报
Acta Pharmaceutica Sinica
; (12): 1511-1516, 2012.
Article
in Zh
| WPRIM
| ID: wpr-274630
Responsible library:
WPRO
ABSTRACT
To explore novel non-opioid analgesic agents, 16 compounds were synthesized and their structures were confirmed by 1H NMR and HR-MS. YX0611-1 was treated as the leading compound. The results of mice writhing model and hot plate model showed that compounds 2, 7, 8, 9, 11 and 15 had obvious analgesic activities in vivo. The test of affinity to mu, delta, kappa receptor displayed that active compounds didn't act on opioid receptor. The results of preliminary toxicity and pharmacokinetic tests showed that compound 7 had better safety and pharmacokinetic properties than that of YX0611-1, and it deserved further development.
Full text:
1
Index:
WPRIM
Main subject:
Pharmacology
/
Piperazines
/
Structure-Activity Relationship
/
Pain Measurement
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Pharmacokinetics
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Random Allocation
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Chemistry
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Receptors, Opioid
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Analgesics, Non-Narcotic
/
Toxicity
Limits:
Animals
Language:
Zh
Journal:
Acta Pharmaceutica Sinica
Year:
2012
Type:
Article