| 词条 | Bucinnazine |
| 释义 |
| verifiedrevid = | IUPAC_name = 1-[4-[(E)-3-Phenylprop-2-enyl]piperazin-1-yl]butan-1-one | image = AP-237.svg | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = PSA | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 17719-89-0 | CAS_supplemental = 17730-82-4 (HCl) | ATC_prefix = | ATC_suffix = | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | PubChem = 6005081 | ChemSpiderID = 4777510 | UNII = J735KL8O54 | synonyms = AP-237 | C=17 | H=24 | N=2 | O=1 | smiles = CCCC(=O)N1CCN(CC1)C/C=C/C2=CC=CC=C2 | StdInChI = 1S/C17H24N2O/c1-2-7-17(20)19-14-12-18(13-15-19)11-6-10-16-8-4-3-5-9-16/h3-6,8-10H,2,7,11-15H2,1H3/b10-6+ | StdInChIKey = ZQBMUHABRSEAIK-UXBLZVDNSA-N }} Bucinnazine (1-butyryl-4-cinnamylpiperazine) is an opioid analgesic drug that was widely used in China to treat pain in cancer patients as of 1986.[1] It is one of the most potent compound among a series of analgesic acyl piperazines compounds first synthesized and reported in Japan in the 1970s.[2][3][4] Bucinnazine has analgesic potency comparable to that of morphine but with a relatively higher therapeutic index. The drug were 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.[5] 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.[1] 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. References1. ^1 {{cite journal | author = Qing T, Zhi-Ji C, and Wei-Ping W. | title = Experimental Study on the Dependence-Producing Properties of Qiang Tong Ding (AP-237) | journal = Chin. J. Clin. Pharmacol. | date = 1986 | issue = 2 | url = http://en.cnki.com.cn/Article_en/CJFDTotal-GLYZ198602003.htm}} 2. ^{{Cite journal | pmid = 4916908| year = 1970| last1 = Nishimura| first1 = N.| title = Clinical exaluation of a new analgesic agent Ap-237| journal = Masui. The Japanese Journal of Anesthesiology| volume = 19| issue = 6| pages = 653–6| last2 = Kiuchi| first2 = M.| last3 = Kanetake| first3 = Y.| last4 = Takahashi| first4 = T.}} 3. ^{{Cite journal | pmid = 1156018| year = 1975| last1 = Carrano| first1 = R. A.| title = Analgesic and tolerance studies with AP-237, a new analgesic| journal = Archives Internationales de Pharmacodynamie et de Therapie| volume = 213| issue = 1| pages = 41–57| last2 = Kimura| first2 = K. K.| last3 = McCurdy| first3 = D. H.}} 4. ^{{Cite journal | pmid = 1156016| year = 1975| last1 = Carrano| first1 = R. A.| title = General pharmacology of a new analgesic-AP-237| journal = Archives Internationales de Pharmacodynamie et de Therapie| volume = 213| issue = 1| pages = 28–40| last2 = Kimura| first2 = K. K.| last3 = Landes| first3 = R. C.| last4 = McCurdy| first4 = D. H.}} 5. ^{{Cite journal | pmid = 8294946| year = 1993| last1 = Barlocco| first1 = D.| title = Computer-aided structure-affinity relationships in a set of piperazine and 3,8-diazabicyclo3.2.1octane derivatives binding to the mu-opioid receptor| journal = Journal of Computer-Aided Molecular Design| volume = 7| issue = 5| pages = 557–71| last2 = Cignarella| first2 = G.| last3 = Greco| first3 = G.| last4 = Novellino| first4 = E.}} 4 : Analgesics|Euphoriants|Mu-opioid agonists|Piperazines |
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