WB-4101 explained

WB-4101 is a compound which acts as an antagonist at the α_1B-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]}

See also

• Phendioxan

Notes and References

1. Green PN, Shapero M, Wilson C . The synthesis and pharmacological properties of a series of 2-substituted aminomethyl-1,4-benzodioxanes . Journal of Medicinal Chemistry . 12 . 2 . 326–9 . March 1969 . 5791620 . 10.1021/jm00302a033 .
2. Morrow AL, Creese I . 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 . April 1986 . 3010073 .
3. Melchiorre C, Bolognesi ML, Budriesi R, Chiarini A, Giardinà D, Minarini A, Quaglia W, Leonardi A . 6 . Search for selective antagonists at alpha 1-adrenoreceptors: neutral or negative antagonism? . Farmaco . 53 . 4 . 278–86 . April 1998 . 9658586 . 10.1016/S0014-827X(98)00022-6 .
4. Melchiorre C, Angeli P, Bolognesi ML, Chiarini A, Giardinà D, Gulini U, Leonardi A, Marucci G, Minarini A, Pigini M, Quaglia W, Rosini M, Tumiatti V . 6 . Alpha 1-adrenoreceptor antagonists bearing a quinazoline or a benzodioxane moiety . Pharmaceutica Acta Helvetiae . 74 . 2–3 . 181–90 . March 2000 . 10812956 . 10.1016/S0031-6865(99)00049-7 .
5. Fumagalli L, Pallavicini M, Budriesi R, Gobbi M, Straniero V, Zagami M, Chiodini G, Bolchi C, Chiarini A, Micucci M, Valoti E . 6 . 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 . December 2012 . 23124215 . 10.1016/j.ejmech.2012.09.049 .
6. Fumagalli L, Pallavicini M, Budriesi R, Bolchi C, Canovi M, Chiarini A, Chiodini G, Gobbi M, Laurino P, Micucci M, Straniero V, Valoti E . 6 . 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 . August 2013 . 23902232 . 10.1021/jm400867d .