(S)-Willardiine ((-)-Willardiine) is a potent agonist of AMPA/kainate receptors with an EC50 value of 45µM [1]. (S)-Willardiine can activate the whole-cell current by activating GluR6(Q)/KA-2 kainate receptors[2]. (S)-Willardiine has been widely used as a model compound to attach various groups to construct related derivatives, thereby exerting the function of the kainate receptor antagonist[3].
References:
[1] Patneau D K, Mayer M L, Jane D E, et al. Activation and desensitization of AMPA/kainate receptors by novel derivatives of willardiine[J]. Journal of Neuroscience, 1992, 12(2): 595-606.
[2] Fukushima T, Marshall J, Sakata K, et al. Calcium inhibits willardiine-induced responses in kainate receptor GluR6 (Q)/KA-2[J]. Neuroreport, 2001, 12(1): 163-167.
[3] Dolman N P, Troop H M, More J C A, et al. Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors[J]. Journal of medicinal chemistry, 2005, 48(24): 7867-7881.
(S)-Willardiine ((-)-Willardiine)是一种强效的AMPA/kainate受体激动剂，EC50值为45μM[1]。(S)-Willardiine 可通过激活GluR6(Q)/KA-2 kainate受体来诱发全细胞电流[2]。(S)-Willardiine已被广泛用作模型化合物，通过连接各种基团来构建相关衍生物，从而发挥kainate受体拮抗剂的功能[3]。