Substance P Receptor Antagonist 1 has the potential function in gastrointestinal disorders, inflammatory diseases, respiratory, and central nervous system disorders.
Vapreotide diacetate is a synthetic analog of somatostatin. It has analgesic activity most likely mediated through the blockade of the neurokinin-1 receptor (NK1R), the substance P (SP)-preferring receptor.
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 +
CP-122721 is an NK1 receptor antagonist with a unique antidepressant, anti-anxiety, and antiemetic properties. It is also an effective selective substance P receptor antagonist.
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......
[Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) 是一种 Substance P 类似物,在大鼠大脑中对神经激肽 1 受体 (NK1R) 的作用与 Substance P 大致相等,但作用时间大大延长。[Glp5,(Me)Phe8,Sar9] Substance P (5-11) 能选择性地激活大鼠大脑间脑和中脑皮层的多巴胺代谢。[Glp5,(Me)Phe8,Sar9] Substance P (5-11) 还可增加大鼠运动活性,诱导成瘾剂寻求行为的恢复。