Proxyfan (Proxifan) is a high-affinity protean antagonist/agonist of histamine H3 receptors with a full spectrum of pharmacological activity ranging from full agonist to full inverse agonist(antagonist), depending on the competition between constitutively active and resting H3 receptors within a given tissue or brain region.Proxyfan acts as a neutral antagonist in the feeding-associated ventral medial nucleus of the hypothalamus, and as a agonist in the basolateral amygdala of the rat (BLA).

Rat H3LR:2.9 nM (Ki), Human H3LR:2.7 nM (Ki)

Proxyfan 是一种组胺 H3 受体的中性拮抗剂（neutral antagonist），其对大鼠和人类 H3 受体的结合常数（Ki 值）分别为 2.9 nM 和 2.7 nM，显示出较高的亲和力。[1]

H3受体中性拮抗剂Proxyfan在大鼠中通过腹腔注射给药。Proxyfan（0.2–5.0 mg/kg）在光照期或黑暗期对自由进食大鼠的摄食量均无影响。在夜间，Proxyfan拮抗了H3受体激动剂Imetit（10 mg/kg）引起的促食欲作用以及反向激动剂Thioperamide（2 mg/kg）引起的抑食作用。[2]