nk1, rat

Vofopitant dihydrochloride (GR 205171A) 是一种可口服且具有选择性的速激肽 NK1 受体拮抗剂，对 [3H]SP 与 NK1 结合有抑制作用， pKi 值分别为 9.5 和 10.6。Vofopitant dihydrochloride 是治疗病理性呕吐的潜在化合物。

Vofopitant (GR 205171) 是一种有效的 NK1 receptor 拮抗剂，具有抗焦虑和止吐活性，可用于研究创伤后应激障碍(PTSD)。

GR203040 inhibits cyclophosphamide-induced damage in the rat and ferret bladder. GR-203040 is a selective NK1 receptor antagonist.

Rolapitant (SCH619734) hydrochloride 是一种高效选择性和具有口服活性的神经激肽 1 (NK1) 受体拮抗剂，Ki 值为 0.66 nM。Rolapitant hydrochloride (Rolapitant HCl) 不与 CYP3A4 产生互作。Rolapitant hydrochloride 在雪貂呕吐模型中显示出强效的中枢介导的止吐活性。

Rolapitant, also known as SCH-619734, is an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy.

Nolpitantium Free Base is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no effect in bioassays for NK2 and NK3 receptors. The antagonism exerted by Nolpitantium toward NK1 receptors was apparently non-competitive, with pD2' values between 9.65 and 10.16 in the different assays. Nolpitantium also blocked in vitro [Sar9, Met(O2)11]substance P-induced release of acetylcholine from rat striatum. In vivo, Nolpitantium exerted highly potent antagonism toward [Sar9, Met(O2)11]substance P-induced hypotension in dogs, bronchoconstriction in guinea-pig) and plasma extrava......

GR 64349为一种有效且高度选择性的神经激肽 2(NK2)受体肽类拮抗剂，具有在大鼠结肠中的EC50值仅为3.7 nM。相较于NK1和NK3受体，GR 64349展现出超过1000倍与300倍的选择性差异。

[Sar9,Met(O2)11]-Substance P TFA is a selective tachykinin NK1 receptor agonist.[Sar9,Met(O2)11]-Substance P and septide (10-100 pmol per rat, i.c.v.) are equipotent in increasing mean arterial blood pressure (MAP) and heart rate (HR), yet they have dissi

[Sar9,Met(O2)11]-Substance P acetate(110880-55-2 free base) 是一种速激肽 NK1 受体选择性激动剂。它是一种选择性速激肽 NK1 受体激动剂。它和 septide（每只大鼠 10-100 pmol，i.c.v.）在增加平均动脉血压 (MAP) 和心率 (HR)，但它们的时间进程不同。两种激动剂都以剂量依赖性方式增加洗脸和吸鼻，而它是一种产生美容效果的化合物。

Potent and selective tachykinin NK2 receptor agonist (EC50 = 3.7 nM in rat colon). Displays > 1000- and > 300-fold selectivity over NK1 and NK3 receptors respectively. Active in vivo.

Scyliorhinin I 是一种作用于速激肽-1 (NK-1) 及速激肽-2 (NK-2) 受体的激动剂.在大鼠颌下腺NK-1受体上的Ki值达到0.9 nM, 而在仓鼠膀胱NK-2受体上的Ki值为2 nM.此外,Scyliorhinin I 还能有效引起豚鼠回肠纵向肌肉的收缩.