| 词条 | 18,19-Dehydrobuprenorphine |
| 释义 |
| ImageFile = 18,19-Dehydrobuprenorphine (HS-599).svg | ImageSize = 200px | ImageAlt = | IUPACName = 17-Cyclopropylmethyl-4,5α-epoxy-6α,14α etheno-7α-(1-hydroxy-1,2,2-trimethylpropyl)-6β-methoxymorphinan-3-ol | OtherNames = HS 599 |Section1={{Chembox Identifiers | CASNo = 155203-05-7 | CASNo_Ref = {{cascite|correct|}} | PubChem =101720618 | StdInChI=1S/C29H39NO4/c1-25(2,3)26(4,32)20-15-27-10-11-29(20,33-5)24-28(27)12-13-30(16-17-6-7-17)21(27)14-18-8-9-19(31)23(34-24)22(18)28/h8-11,17,20-21,24,31-32H,6-7,12-16H2,1-5H3/t20-,21-,24-,26+,27+,28+,29?/m1/s1 | StdInChIKey = XXEUUFWMPBSHCE-NFCPXPRCSA-N | SMILES = C[C@]([C@H]1C[C@]23C=CC1([C@H]4[C@@]25CCN([C@@H]3CC6=C5C(=C(C=C6)O)O4)CC7CC7)OC)(C(C)(C)C)O |Section2={{Chembox Properties | C=29 | H=39 | N=1 | O=4 | Appearance = | Density = | MeltingPt = | BoilingPt = | Solubility = }} |Section3={{Chembox Hazards | MainHazards = | FlashPt = | AutoignitionPt = }} }}18,19-Dehydrobuprenorphine (HS-599) is a {{Not a typo|didehydro}} derivative of buprenorphine. It has about twice the potency of buprenorphine. It has produced a long-lasting antinociceptive response in animal tests.[1] 18,19-Dehydrobuprenorphine never induced conditioned place-preference in test animals, unlike buprenorphine and morphine.[1] 18,19-Dehydrobuprenorphine has about three times higher affinity for the μ-opioid receptor but lower affinity for δ- and κ-opioid receptors when compared with buprenorphine.[1][2] References1. ^1 2 {{cite journal| pmc=1572965 | pmid=11564664 | doi=10.1038/sj.bjp.0704280 | volume=134 | title=HS-599: a novel long acting opioid analgesic does not induce place-preference in rats | journal=Br J Pharmacol | pages=441–7 | last1 = Lattanzi | first1 = R | last2 = Negri | first2 = L | last3 = Giannini | first3 = E | last4 = Schmidhammer | first4 = H | last5 = Schutz | first5 = J | last6 = Improta | first6 = G}} {{Opioidergics}}{{DEFAULTSORT:Dehydrobuprenorphine, 18,19-}}{{analgesic-stub}}2. ^[https://web.archive.org/web/20130523174347/http://www.scribd.com/doc/38715674/Synthesis-and-Pharmacological-Evaluation-of-18-19-Dehydrobuprenorphine-Heterocycles-2001-54-989-998-DOI-10-3987-COM-00-S-I-46-http-dx-doi-o SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF18,19-DEHYDROBUPRENORPHINE] Archive.org 3 : Oripavines|Semisynthetic opioids|Morphinans |
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