| 词条 | 3-Bromocytisine |
| 释义 |
| IUPAC_name = (1R,5S)-9-Bromo-1,2,3,4,5,6-hexahydro-1,5-methano-8H-pyrido[1,2-a][1,5]diazocin-8-one | image = 3-bromocytisine_structure.png | tradename = | pregnancy_category = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = 207390-14-5 | ATC_prefix = | ATC_suffix = | PubChem = 15519735 | ChemSpiderID = 21376088 | C=11 | H=13 | Br=1 | N=2 | O=1 | molecular_weight = 269.14 g/mol | smiles = c1cc2n(c(=O)c1Br)C[C@H]3C[C@@H]2CNC3 | StdInChI = 1S/C11H13BrN2O/c12-9-1-2-10-8-3-7(4-13-5-8)6-14(10)11(9)15/h1-2,7-8,13H,3-6H2/t7-,8+/m0/s1 | StdInChIKey = DWDCLEHDNICBMI-JGVFFNPUSA-N }}3-Bromocytisine is a derivative of the toxic alkaloid cytisine that acts as a highly potent agonist at neural nicotinic acetylcholine receptors, binding primarily to the α4β2 and α7 subtypes. 3-Bromocytisine is a full agonist at the α7 subtype while it is only a partial agonist at α4β2, but has an extremely strong binding affinity at α4β2 with 200-fold selectivity for α4β2 over α7. In animal studies 3-bromocytisine stimulates the release of dopamine and noradrenaline and increases locomotor activity.[1][2][3][4] References1. ^{{Cite journal | doi = 10.1016/S0223-5234(01)01222-3 | last1 = Imming | first1 = P. | last2 = Klaperski | first2 = P. | last3 = Stubbs | first3 = M. T. | last4 = Seitz | first4 = G. | last5 = Gündisch | first5 = D. | title = Syntheses and evaluation of halogenated cytisine derivatives and of bioisosteric thiocytisine as potent and selective nAChR ligands | journal = European Journal of Medicinal Chemistry | volume = 36 | issue = 4 | pages = 375–388 | year = 2001 | pmid = 11461763}} {{Cholinergics}}{{DEFAULTSORT:Bromocytisine, 3-}}{{nervous-system-drug-stub}}2. ^{{Cite journal | doi = 10.1046/j.1471-4159.2001.00481.x | last1 = Houlihan | first1 = L. M. | last2 = Slater | first2 = Y. | last3 = Guerra | first3 = D. L. | last4 = Peng | first4 = J. H. | last5 = Kuo | first5 = Y. P. | last6 = Lukas | first6 = R. J. | last7 = Cassels | first7 = B. K. | last8 = Bermudez | first8 = I. | title = Activity of cytisine and its brominated isosteres on recombinant human alpha7, alpha4beta2 and alpha4beta4 nicotinic acetylcholine receptors | journal = Journal of Neurochemistry | volume = 78 | issue = 5 | pages = 1029–1043 | year = 2001 | pmid = 11553677}} 3. ^{{Cite journal | last1 = Abin-Carriquiry | first1 = J. A. S. | last2 = Voutilainen | first2 = M. H. | last3 = Barik | first3 = J. | last4 = Cassels | first4 = B. K. | last5 = Iturriaga-Vásquez | first5 = P. | last6 = Bermudez | first6 = I. | last7 = Durand | first7 = C. | last8 = Dajas | first8 = F. | last9 = Wonnacott | first9 = S. | doi = 10.1016/j.ejphar.2006.02.012 | title = C3-halogenation of cytisine generates potent and efficacious nicotinic receptor agonists | journal = European Journal of Pharmacology | volume = 536 | issue = 1–2 | pages = 1–11 | year = 2006 | pmid = 16563372 | pmc = }} 4. ^{{Cite journal | last1 = Abin-Carriquiry | first1 = J. A. S. | last2 = Urbanavicius | first2 = J. | last3 = Scorza | first3 = C. | last4 = Rebolledo-Fuentes | first4 = M. | last5 = Wonnacott | first5 = S. | last6 = Cassels | first6 = B. K. | last7 = Dajas | first7 = F. | doi = 10.1016/j.ejphar.2010.02.030 | title = Increase in locomotor activity after acute administration of the nicotinic receptor agonist 3-bromocytisine in rats | journal = European Journal of Pharmacology | volume = 634 | issue = 1–3 | pages = 89–94 | year = 2010 | pmid = 20184877 | pmc = }} 4 : Nicotinic agonists|Nitrogen heterocycles|Lactams|Organobromides |
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