neurokinin-1 (nk1) receptor

Physalaemin is a non-mammalian tachykinin.

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。

N-Acetyl-L-tryptophan (N-acetyltryptophan) 是内源性代谢产物的一种。

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。

Tradipitant (VLY-686) 是一种有效的神经激肽-1 拮抗剂。

Fosaprepitant dimeglumine (MK-0517) 是 Aprepitant 的前药。它是一种神经激肽 1 受体拮抗剂，可用于预防化疗引起的恶心呕吐。

Physalaemin acetate 是一种非哺乳动物速激肽，在选择性结合神经激肽 1 (NK1) 受体时具有高亲和力。

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)。

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 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......

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

Hemokinin 1, human TFA 是选择性的速激肽神经激肽 1 (NK1) 受体完全激动剂。Hemokinin 1, human TFA 也是 NK2和 NK3受体的完全激动剂。Hemokinin 1, human TFA 可以产生非阿片样物质的缓解疼痛作用。

CP 122721 hydrochloride是一种有效的非肽选择性neurokinin NK1非肽拮抗剂，针对IM-9细胞中表达的人NK1受体展示出9.8的pIC50值，具备抗焦虑和抗抑郁样效应。

Fosaprepitant-d4 Dimeglumine 是 Fosaprepitant Dimeglumine 的氘代化合物。Fosaprepitant Dimeglumine 的 CAS 号为 265121-04-8。Fosaprepitant dimeglumine 是 Aprepitant 的前药。它是一种神经激肽 1 受体拮抗剂，可用于预防化疗引起的恶心呕吐。

Hemokinin 1 (mouse) acetate(208041-90-1 free base) 是一种选择性兴奋剂 1 受体激动剂，对人 NK1 受体的 Ki 值为 0.175 nM，对人 NK2 受体的 Ki 值为 560 nM。

Hemokinin 1 (human) acetate(491851-53-7 free base) 是一种内源性 P 物质同系物，是速激肽 NK1 受体的选择性激动剂（NK1、NK3 和 NK2 受体的 IC50 值分别为 1.8、370 和 480 nM）。在体外对 B 细胞具有增殖和抗凋亡作用，在体内具有抗高血压作用。