substance p receptor antagonist 1

Substance P Receptor Antagonist 1 has the potential function in gastrointestinal disorders, inflammatory diseases, respiratory, and central nervous system disorders.

Lanepitant 2HCl 是一种非肽类神经激肽-1 受体拮抗剂，具有镇痛和抗炎活性。Lanepitant 2HCl 抑制 P 物质与神经激肽-1 受体的结合，抑制神经源性炎症和疼痛传递，可用于研究偏头痛等疼痛性神经病变类疾病。

Aprepitant 是选择性和高亲和力的神经激肽1受体拮抗剂，Kd 值为86 pM。

YM49598 is a tachykinin receptor antagonist. YM49598 exhibited high binding affinities at NK(1) (pK(i) = 9.09 + - 0.02) and NK(2) (pK(i) = 9.94 + - 0.03) receptors, respectively. YM49598 was almost inactive but produced a potent inhibition (IC(50) = 11 +

Maropitant citrate 是一种合成的神经激肽-1 受体拮抗剂和 P 物质抑制剂，可用于控制猫狗的呕吐。

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。

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, 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......

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。

[D-Trp2,7,9] Substance P 是一种速激肽 (Neurokinin Receptor) 拮抗剂，对 NK-1、NK-2和 NK-3受体的 Ki 值分别为 1 μM、1.3 μM 和 ~9 μM。

(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B 是 Neurokinin B(Neurokinin Receptor) 的竞争性拮抗剂，pA2 为 5.5，对 Substance P 或 Neurokinin A 没有影响。

(D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P 是一种选择性的 NK1receptor 拮抗剂。

Substance P(1-4) Acetate 是一种神经激肽受体(NK-R)拮抗剂，抑制 PV EEC 的形成，影响 PV CD36 + 红系祖细胞增殖和分化。

SLV-317,作为一种口服活性的神经激肽-1受体拮抗剂,能够有效抵抗P物质所引发的生理效应.