| dbo:abstract |
Bucinnazine (AP-237, 1-butyryl-4-cinnamylpiperazine) is an opioid analgesic drug that was widely used in China to treat pain in cancer patients as of 1986. It is one of the most potent compounds among a series of piperazine-amides first synthesized and reported in Japan in the 1970s. Bucinnazine has analgesic potency comparable to that of morphine but with a relatively higher therapeutic index. The drug was initially claimed to be a non-narcotic analgesic. However, subsequent studies have shown bucinnazine and similar acyl piperazines to be potent and selective agonists of μ-opioid receptor (MOR) with relatively low affinity for the δ-opioid receptor and the κ-opioid receptor. In accordance with these studies, results from the intravenous self-administration experiments in rats showed that bucinnazine has a marked reinforcing effect with tolerance and dependence quickly developing. In addition, the morphine antagonist naloxone reverses the effect of bucinnazine and precipitates withdrawal symptoms in bucinnazine treated rats further indicating a mechanism of analgesia mediated via selective agonist activity at μ-opioid receptors. (en) |
| dbo:casNumber |
17719-89-0 17730-82-4 (HCl) |
| dbo:fdaUniiCode |
J735KL8O54 |
| dbo:pubchem |
6005081 |
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https://pubchem.ncbi.nlm.nih.gov/compound/6447698 |
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PSA (en) |
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ZQBMUHABRSEAIK-UXBLZVDNSA-N (en) |
| dbp:synonyms |
AP-237 (en) |
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J735KL8O54 (en) |
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| rdfs:comment |
Bucinnazine (AP-237, 1-butyryl-4-cinnamylpiperazine) is an opioid analgesic drug that was widely used in China to treat pain in cancer patients as of 1986. It is one of the most potent compounds among a series of piperazine-amides first synthesized and reported in Japan in the 1970s. Bucinnazine has analgesic potency comparable to that of morphine but with a relatively higher therapeutic index. (en) |
| rdfs:label |
Bucinnazine (en) |
| owl:sameAs |
wikidata:Bucinnazine https://global.dbpedia.org/id/2YraK |
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wikipedia-en:Bucinnazine?oldid=1102179564&ns=0 |
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