1. GPCR/G Protein
    Neuronal Signaling
  2. Neurokinin Receptor

Neurokinin Receptor

There are three main classes of neurokinin receptors: NK1R (the substance P preferring receptor), NK2R, and NK3R。 These tachykinin receptors belong to the class I (rhodopsin-like) G-protein coupled receptor (GPCR) family。 The various tachykinins have different binding affinities to the neurokinin receptors: NK1R, NK2R, and NK3R。 These neurokinin receptors are in the superfamily of transmembrane G-protein coupled receptors (GPCR) and contain seven transmembrane loops。 Neurokinin-1 receptor interacts with the Gαq-protein and induces activation of phospholipase C followed by production of inositol triphosphate (IP3) leading to elevation of intracellular calcium as a second messenger。 Further, cyclic AMP (cAMP) is stimulated by NK1R coupled to the Gαs-protein。 The neurokinin receptors are expressed on many cell types and tissues。

Neurokinin Receptor 相关产品 (42):

Cat. No. Product Name Effect Purity
  • HY-10052
    Aprepitant Inhibitor 99.93%
    Aprepitant (MK-0869) 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。
  • HY-P0201
    Substance P Modulator 98.07%
    Substance P 是一种神经肽,作为神经递质和神经调节剂。Substance P 的内源性受体是神经激肽1受体 (neurokinin 1 receptorNK1R)。
  • HY-15722
    SB-222200 Antagonist 99.91%
    SB 222200是可逆的竞争性人NK受体抑制剂,对hNK-3受体的Ki为4.4 nM,能透过血脑屏障。
  • HY-14751
    Rolapitant Antagonist 98.01%
    Rolapitant (SCH619734)是高效选择性具有口服活性的 neurokinin NK1 受体抑制剂,Ki值为0.66 nM。
  • HY-19632
    Fezolinetant Antagonist 98.29%
    Fezolinetant 是一种神经激肽-3 受体 (neurokinin 3 receptor) 拮抗剂,可用于更年期潮热的研究。
  • HY-P1012
    [Sar9,Met(O2)11]-Substance P Agonist 98.45%
    [Sar9,Met(O2)11]-Substance P 是一种选择性的速激肽 NK1 受体激动剂。
  • HY-16346
    Netupitant Antagonist 99.78%
    Netupitant (CID-6451149) 是一高效、选择性、口服活性的Neurokinin-1受体(NK1)拮抗剂,Ki值为0.95nM。
  • HY-14407A
    Fosaprepitant dimeglumine Antagonist >99.0%
    Fosaprepitant dimeglumine(MK-0517)是神经激肽-1受体拮抗剂,可作用于化疗引起的恶心呕吐。
  • HY-14432
    Pavinetant Antagonist 99.74%
    Pavinetant (MLE-4901) 是一种神经激肽-3 受体 (NK3R) 拮抗剂。
  • HY-P0187
    Senktide Agonist 99.56%
    Senktide 是一种速激肽 NK3 受体激动剂。
  • HY-10053
    Maropitant Antagonist 99.00%
    Maropitant是神经激肽(NK1)受体拮抗剂。
  • HY-18006
    NKP608 Antagonist 99.34%
    NKP608为非肽类4-氨基哌啶衍生物,是神经激肽-1(NK-1)受体拮抗剂,IC50为2.6 nM。
  • HY-P1031
    [bAla8]-Neurokinin A(4-10) Agonist 98.17%
    [bAla8]-Neurokinin A(4-10) 是一种神经激肽-2 受体 (neurokinin 2 receptor) 激动剂。
  • HY-P1485
    Substance P 1-7
    Substance P (7-11) 是神经肽P物质 (SP) 的片段。Substance P (7-11) 可对孤束核产生抑制和缓和作用。
  • HY-16346S
    Netupitant D6 Antagonist
    Netupitant D6是Netupitant(CID-6451149)氘代化合物标准品。
  • HY-12114
    Serlopitant Antagonist
    Serlopitant是一种选择性的 神经激肽-1 (NK-1) 受体拮抗剂。
  • HY-P1485A
    Substance P (1-7)(TFA) 99.20%
    Substance P (1-7)(TFA) 是神经肽 P 物质 (SP) 的片段。Substance P (1-7)(TFA) 可对孤束核产生抑制和缓和作用。
  • HY-101704
    Y1 receptor antagonist 1 Antagonist
    Y1 receptor antagonist 1 是 H-409/22 的一个异构体,是神经肽 (neuropeptide Y1) 受体拮抗剂。
  • HY-14552
    Talnetant Antagonist 99.27%
    Talnetant (SB 223412)是高活性NK3受体选择性拮抗剂,Ki为1.4 nM,比对hNK-2受体的抑制性高100倍,对hNK-1无亲和性。
  • HY-14407
    Fosaprepitant Antagonist
    Fosaprepitant(L-758298)是神经激肽-1受体水溶性拮抗剂,可作用于化疗引起的恶心呕吐。
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