[Synthesis and central none-opioid analgesic activity of SIPI5047].
Compound SIPI5047 was synthesize by using piperazine as starting material in five reaction steps, and its central none-opioid analgesic activity was studied. Its analgesic activity, pharmacological mechanism, action type and drug dependence were well studied in vivo and in vitro. The results show that SIPI5047 has potent analgesic activities in vivo, which is quite similar to morphine and also much more powerful than paracetamol. SIPI5047 has no efficacy to reduce fever or inflammation, but has an obvious action on central nervous system. SIPI5057 has no apparent affinity with the mu-receptor and it is an antagonist that acts on the polyamine site of the NMDA receptor. SIPI5057 appears no drug dependence. SIPI5047 is a novel central none-opioid analgesic agent and more worthy of further research as a new drug candidate.
Li
Jian-Qi
JQ
Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China. lijq@sipi.com.cn
Huang
Li-Ying
LY
Chen
Xin-Jian
XJ
Weng
Zhi-Jie
ZJ
Zhang
Chun-Nian
CN
D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D005260:Female; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010147:Pain Measurement / Q000379:methods*; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D011897:Random Allocation; D051381:Rats; D017207:Rats, Sprague-Dawley; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors; D017450:Receptors, Opioid, mu / Q000378:metabolism; D019966:Substance-Related Disorders / Q000209:etiology
D000700:Analgesics; D010879:Piperazines; D016194:Receptors, N-Methyl-D-Aspartate; D017450:Receptors, Opioid, mu