| 词条 | BU09059 |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = ethyl 2[(3R)-7-hydroxy-1,2,3,4-tetrahydroisoquinolin-3-yl]formamido3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]propanoate | image = BU09059.svg | width = | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = | CAS_supplemental = | ATC_prefix = | ATC_suffix = | PubChem = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = | C=28 | H=37 | N=3 | O=5 | molecular_weight = | smiles = CCOC(=O)C(CN1CC[C@](C)([C@@H](C)C1)c2cccc(O)c2)NC(=O)[C@H]3Cc4ccc(O)cc4CN3 | StdInChI_Ref = | StdInChI = 1S/C28H37N3O5/c1-4-36-27(35)25(30-26(34)24-13-19-8-9-23(33)12-20(19)15-29-24)17-31-11-10-28(3,18(2)16-31)21-6-5-7-22(32)14-21/h5-9,12,14,18,24-25,29,32-33H,4,10-11,13,15-17H2,1-3H3,(H,30,34)/t18-,24+,25?,28+/m0/s1 | StdInChIKey_Ref = | StdInChIKey = RKGRJMYCISUSNK-XTNINKNLSA-N | synonyms = }}BU09059 is a potent, selective, short-acting (non-"inactivating") antagonist of the κ-opioid receptor (KOR).[1][2] It was derived from the irreversible (long-acting) KOR antagonist JDTic in search of an antagonist with a reversible profile of inactivation of the KOR that could be used with less concern to treat psychiatric disorders.[1][2] In addition to its reversibility, BU09059 is much more selective for the KOR than JDTic, showing 15-fold and 616-fold preference for the KOR over the μ- and δ-opioid receptors (Ki = 1.72 nM, 26.5 nM, and 1060 nM, respectively).[1] See also
References1. ^1 2 {{cite journal | first1=Joseph J. | last1=Casal-Dominguez | title=Characterization of BU09059: A Novel Potent Selective κ-Receptor Antagonist | last2=Furkert | first2=Daniel | last3=Ostovar | first3=Mehrnoosh | last4=Teintang | first4=Linnea | last5=Clark | first5=Mary J. | last6=Traynor | first6=John R. | last7=Husbands | first7=Stephen. M. | last8=Bailey | first8=Sarah J. | journal=ACS Chemical Neuroscience | date=March 2014 | volume=5 | issue=3 | pages=177–184 | issn=1948-7193 | doi=10.1021/cn4001507 | pmid=24410326 | pmc=3963132}} {{Opioid receptor modulators}}{{nervous-system-drug-stub}}2. ^1 {{cite journal | first1=Mariangela | last1=Urbano | url=http://www.sciencedirect.com/science/article/pii/S0960894X14002674 | title=Antagonists of the kappa opioid receptor | last2=Guerrero | first2=Miguel | last3=Rosen | first3=Hugh | last4=Roberts | first4=Edward | journal=Bioorganic & Medicinal Chemistry Letters | date=May 2014 | volume=24 | issue=9 | pages=2021–2032 | issn=0960-894X | doi=10.1016/j.bmcl.2014.03.040 | pmid=24690494}} 3 : Kappa antagonists|Opioid antagonists|Synthetic opioids |
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