neurokinin receptors

SSR-241586 is a neurokinin receptors antagonist,and is shown to be active in the treatment of depression, schizophrenia, urinary trouble, emesis, and irritable bowel syndrome (IBS).

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。

Saredutant(SR 48968,沙瑞度坦)是一种选择性的神经激肽-2（NK2）受体拮抗剂通过阻断 NK2 受体来抑制神经激肽 A 的作用，从而发挥抗抑郁和抗焦虑的效果。

gamma-preprotachykinin amide (72-92) acetate 是一种 21 个氨基酸的肽，属于速激肽 (TK) 家族，在其 C 末端序列中包括神经激肽 A (NKA)。它对中枢 NK-2 受体的亲和力高于 NKA；它对 NK-1 受体的亲和力较低，但是，它有效地刺激唾液分泌，这是由 NK-1 受体激活介导的。

Tachykinin antagonist 1 is an antagonist of neurokinin receptors.

CS-003 free base (CS-003) is a triple tachykinin receptor antagonist with high affinity for human (neurokinin) NK1, NK2 and NK3 receptors, with Ki values of 2.3 nM and 0.54 nM, respectively And 0.74 nM. CS-003 free base (CS-003) has therapeutic effects on

DNK 333 是一种针对神经激肽NK1 NK2受体的双重拮抗剂。

GSK256471 is a potent selective NK(3) antagonist that shows a high affinity for recombinant human (PK (I) value 8.9) and native guinea pig (PK (I) value 8.4) tachykinin NK(3) receptors. In vitro functional assessment showed that GSK256471 reduced the E(Ma

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.

Elizanetant 是有效的神经激肽受体拮抗剂，在精神分裂症研究中有价值。

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.

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。

[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。

Substance P(1-4)为一有效的神经激肽受体(NK-R)拮抗剂，具有调节正常造血功能并抑制内源性红细胞集落(EEC)形成的能力。

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。

Neurokinin B TFA, a member of the tachykinin family, binds to a series of GPCRs, including neurokinin receptors 1 (NK1R), NK2R, and NK3R, to modulate their biological effects.

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.