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

Lanepitant 2HCl is a non-peptide neurokinin-1 receptor antagonist with analgesic and anti-inflammatory activity.Lanepitant 2HCl inhibits the binding of Substance P to the neurokinin-1 receptor, inhibits neurogenic inflammation and pain transmission, and can be used in the study of painful neuropathic disorders, such as migraines.

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.

Spantide I TFA, a selective NK1 receptor antagonist and a substance P analog, exhibits K(i) values of 230 nM for NK1 and 8150 nM for NK2 receptors, respectively. It offers a method to decrease type 1 while increasing type 2 cytokine IL-10 in the infected cornea, significantly reducing corneal perforation [1] [2] [3].

[D-Trp2,7,9] Substance P is a tachykinin (Neurokinin Receptor) antagonist that exhibits inhibitory affinities (K_i values) of 1 μM for NK-1, 1.3 μM for NK-2, and approximately 9 μM for NK-3 receptors [1].

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......

Rolapitant (SCH619734) Hydrochloride is the hydrochloride salt form of rolapitant, 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. Compared to other NK1-receptor antagonists, rolapitant has both a more rapid onset of action and a much longer half-life.

(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B functions as a competitive antagonist to the Neurokinin B receptor, exhibiting a pA2 value of 5.5. Notably, it does not affect Substance P or Neurokinin A [1].

(D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P is a selective NK 1 receptor antagonist [1] .

Aprepitant (Aprepitant`) is a Substance P/Neurokinin-1 Receptor Antagonist. The mechanism of action of aprepitant is as a Neurokinin 1 Antagonist, and Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 2C9 Inducer, and Cytochrome P450 3A4 Inducer.

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 +/

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.