WB-4101 is a compound which acts as an antagonist at the α1B-adrenergic receptor. It was one of the first selective antagonists developed for this receptor and was invented in 1969, but is still commonly used in research into adrenergic receptors, especially as a lead compound from which to develop more selective drugs.[1][2][3][4][5][6]
^Green PN, Shapero M, Wilson C (March 1969). "The synthesis and pharmacological properties of a series of 2-substituted aminomethyl-1,4-benzodioxanes". Journal of Medicinal Chemistry. 12 (2): 326–9. doi:10.1021/jm00302a033. PMID 5791620.
^Morrow AL, Creese I (April 1986). "Characterization of alpha 1-adrenergic receptor subtypes in rat brain: a reevaluation of [3H]WB4104 and [3H]prazosin binding". Molecular Pharmacology. 29 (4): 321–30. PMID 3010073.
^Melchiorre C, Bolognesi ML, Budriesi R, Chiarini A, Giardinà D, Minarini A, et al. (April 1998). "Search for selective antagonists at alpha 1-adrenoreceptors: neutral or negative antagonism?". Farmaco. 53 (4): 278–86. doi:10.1016/S0014-827X(98)00022-6. PMID 9658586.
^Melchiorre C, Angeli P, Bolognesi ML, Chiarini A, Giardinà D, Gulini U, et al. (March 2000). "Alpha 1-adrenoreceptor antagonists bearing a quinazoline or a benzodioxane moiety". Pharmaceutica Acta Helvetiae. 74 (2–3): 181–90. doi:10.1016/S0031-6865(99)00049-7. PMID 10812956.
^Fumagalli L, Pallavicini M, Budriesi R, Gobbi M, Straniero V, Zagami M, et al. (December 2012). "Affinity and activity profiling of unichiral 8-substituted 1,4-benzodioxane analogues of WB4101 reveals a potent and selective α1B-adrenoceptor antagonist". European Journal of Medicinal Chemistry. 58: 184–91. doi:10.1016/j.ejmech.2012.09.049. PMID 23124215.
^Fumagalli L, Pallavicini M, Budriesi R, Bolchi C, Canovi M, Chiarini A, et al. (August 2013). "6-methoxy-7-benzofuranoxy and 6-methoxy-7-indolyloxy analogues of 2-[2-(2,6-Dimethoxyphenoxy)ethyl]aminomethyl-1,4-benzodioxane (WB4101):1 discovery of a potent and selective α1D-adrenoceptor antagonist". Journal of Medicinal Chemistry. 56 (16): 6402–12. doi:10.1021/jm400867d. PMID 23902232.
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4101, compound, which, acts, antagonist, α1b, adrenergic, receptor, first, selective, antagonists, developed, this, receptor, invented, 1969, still, commonly, used, research, into, adrenergic, receptors, especially, lead, compound, from, which, develop, more, . WB 4101 is a compound which acts as an antagonist at the a1B adrenergic receptor It was one of the first selective antagonists developed for this receptor and was invented in 1969 but is still commonly used in research into adrenergic receptors especially as a lead compound from which to develop more selective drugs 1 2 3 4 5 6 WB 4101IdentifiersIUPAC name 2 2 6 Dimethoxyphenoxyethyl aminomethyl 1 4 benzodioxaneCAS Number613 67 2 YPubChem CID5685IUPHAR BPS499ChemSpider5483UNIIE9H51OIT2BCompTox Dashboard EPA DTXSID1043885Chemical and physical dataFormulaC 19H 23N O 5Molar mass345 389 g mol 13D model JSmol Interactive imageSMILES COc1cccc c1OCCNCC2COc3ccccc3O2 OCInChI InChI 1S C19H23NO5 c1 21 17 8 5 9 18 22 2 19 17 23 11 10 20 12 14 13 24 15 6 3 4 7 16 15 25 14 h3 9 14 20H 10 13H2 1 2H3Key GYSZUJHYXCZAKI UHFFFAOYSA NSee also EditPhendioxanReferences Edit Green PN Shapero M Wilson C March 1969 The synthesis and pharmacological properties of a series of 2 substituted aminomethyl 1 4 benzodioxanes Journal of Medicinal Chemistry 12 2 326 9 doi 10 1021 jm00302a033 PMID 5791620 Morrow AL Creese I April 1986 Characterization of alpha 1 adrenergic receptor subtypes in rat brain a reevaluation of 3H WB4104 and 3H prazosin binding Molecular Pharmacology 29 4 321 30 PMID 3010073 Melchiorre C Bolognesi ML Budriesi R Chiarini A Giardina D Minarini A et al April 1998 Search for selective antagonists at alpha 1 adrenoreceptors neutral or negative antagonism Farmaco 53 4 278 86 doi 10 1016 S0014 827X 98 00022 6 PMID 9658586 Melchiorre C Angeli P Bolognesi ML Chiarini A Giardina D Gulini U et al March 2000 Alpha 1 adrenoreceptor antagonists bearing a quinazoline or a benzodioxane moiety Pharmaceutica Acta Helvetiae 74 2 3 181 90 doi 10 1016 S0031 6865 99 00049 7 PMID 10812956 Fumagalli L Pallavicini M Budriesi R Gobbi M Straniero V Zagami M et al December 2012 Affinity and activity profiling of unichiral 8 substituted 1 4 benzodioxane analogues of WB4101 reveals a potent and selective a1B adrenoceptor antagonist European Journal of Medicinal Chemistry 58 184 91 doi 10 1016 j ejmech 2012 09 049 PMID 23124215 Fumagalli L Pallavicini M Budriesi R Bolchi C Canovi M Chiarini A et al August 2013 6 methoxy 7 benzofuranoxy and 6 methoxy 7 indolyloxy analogues of 2 2 2 6 Dimethoxyphenoxy ethyl aminomethyl 1 4 benzodioxane WB4101 1 discovery of a potent and selective a1D adrenoceptor antagonist Journal of Medicinal Chemistry 56 16 6402 12 doi 10 1021 jm400867d PMID 23902232 This pharmacology related article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title WB 4101 amp oldid 1119900771, wikipedia, wiki, book, books, library,
