nk1 antagonist 1

NK-1 Antagonist 1 is a NK-1 receptor antagonist.

NK1receptor antagonist 2 是一种 NK1受体拮抗剂。NK1receptor antagonist 2 可用于耳鸣和听力损失的研究。

Ezlopitant (CJ-11974) 是一种基于喹啉的原型 NK1受体拮抗剂 CP-96345的衍生物。

Netupitant (CID 6451149) 是一种高效选择性、可口服的神经激肽 1 受体 (NK1) 拮抗剂，具有止吐作用，在 CHO 细胞中对 hNK1的 Ki 值为 0.95 nM。

Casopitant mesylate (GW679769B) is a selective, brain permeable, and orally active antagonist of neurokinin 1 (NK1) receptor. It is a second in the class of antiemetics.

Vapreotide is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM).

Vapreotide acetate (BMY-41606 acetate) 是神经激肽-1 (NK1) 受体拮抗剂，IC50值为 330 nM。

Fosrolapitant 作为一种神经激肽 1 (NK1) 受体拮抗剂，具有特定的药理作用。

Casopitant (GW679769) 是一种口服有效的神经激肽-1 (NK1) 受体拮抗剂，用于研究化疗引起的恶心和呕吐 (CINV) 以及术后恶心和呕吐 (PONV)。

TAK-637 is a tachykinin 1 (NK1) receptor antagonist.

Rolapitant (SCH619734) 是一种高效选择性具有口服活性的神经激肽 1 受体抑制剂，Ki 值为0.66 nM。

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。

Benzomalvin B is a fungal metabolite originally isolated from Penicillium. It acts as an antagonist of neurokinin-1 (NK1) receptors, inhibiting binding of substance P by 24% in vitro when used at a concentration of 100 μg ml.

Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor inhibiting binding of substance P by 46% when used at 100 μg ml in vitro. It is also a weak inhibitor of indolamine 2,3-dioxygenase (IDO) with an IC50 value of 130 μM for recombinant IDO. It was isolated from Penicillium and contains an epoxide group at C-19 and C-20, which is not present in benzomalvins A, B, or E.

Rolapitant Hydrochloride is the hydrochloride salt form of rolapitant, an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity.

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......

Acetylaszonalenin is a fungal metabolite that has been found in A. flavipes.1 It acts as an antagonist of neurokinin-1 (NK1) receptors, inhibiting binding of substance P with a Ki value of 170 μM.

WIN 66306 is a cyclic heptapeptide antagonist of neurokinin-1 (NK1) and NK2 receptors originally isolated from A. flavipes. It binds to NK1 and NK2 receptors and inhibits contractions induced by substance P in isolated guinea pig ileum in a concentration-dependent manner.

Imnopitant dihydrochloride 是一种神经激肽NK1受体拮抗剂。

Spantide I TFA 是substance P 的类似物，是选择性的神经激肽-1 受体 (NK1receptor) 的拮抗剂，其对NK1和NK2受体的Ki 值分别为 230 nM 和8150 nM。Spantide I 可减少感染角膜的1型细胞因子和增强2型细胞因子IL-10，从而显著减少角膜穿孔。

GR 94800 TFA 是有效的、选择性的神经激肽 2(NK2)受体的肽类拮抗剂，其对 NK2、NK1和 NK3受体的 pKB 值分别为 9.6、6.4 和 6.0。

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。

[D-Pro4,D-Trp7,9,Nle11] Substance P (4-11) 为高效的神经激肽 NK1 拮抗剂，能够有效抑制金蛋白 P 物质 (GPSP) 与 P 物质 (SP) 的活性。