hnk2

GR 159897 is a competitive, brain-penetrated non-peptide NK2 receptor antagonist with anti-tumor effects. GR 159897 inhibits binding of [3H]GR100679 to human NK2-CHO cells and rat colon membranes (pKis: 9.51 and 10, respectively). It can antagonize bronch

SB 218795 是一种有效的特异性 NK3 拮抗剂，对 hNK3 的 Ki 为 13 nM，比 hNK2 和 hNK1 的特异性高约 90 倍和 7000 倍。

RO-5328673 is a dual NK2 NK3 antagonist. O5328673. [(3)H]RO5328673 bound to a single saturable site on hNK2, hNK3 and gpNK3 with high-affinity. RO5328673 acted as an insurmountable antagonist at both human and guinea-pig NK3 receptors in the [(3)H]IP accumulation assay. In binding kinetic analyses, [(3)H]RO5328673 had fast association and dissociation rates at hNK2 while it had a fast association rate and a remarkably slow dissociation rate at gp and hNK3. In electrophysiological recordings of gp SNpc, RO5328673 inhibited the senktide-induced potentiation of spontaneous activity of dopaminergic neurons with an insurmountable mechanism of action. RO5328673 exhibited in-vivo activity in gerbils, robustly reversing the senktide-induced locomotor activity.