NK2R Antagonist

Saredutant is a selective NK2 receptor antagonist.

GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK₂) receptor antagonist. GR 159897 has little or no affinity for NK₁ and NK₃ receptors. GR 159897 inhibits binding of [³H]GR100679 to human NK₂ (hNK₂)-CHO cells and rat colon membranes with pK_is of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects.

L-659874 is a selective NK2 receptor antagonist with an IC₅₀ value of 0.49 μM in hamsters. L-659874 inhibits NK2 receptor-mediated hydrolysis of inositol phospholipids. L-659874 could be used for research on the correlation between pain signal transduction and smooth muscle responses.

RO5328673 is an orally active, blood-brain barrier permeable neurokinin receptor antagonist that effectively targets human NK3 receptors (K_i=0.4 nM, K_a=0.1 nM), human NK2 receptors (K_i=1.1 nM, K_a=0.9 nM), and guinea pig NK3 receptors (K_a=0.1 nM and 0.13 nM). RO5328673 acts as an insurmountable antagonist of NK3 receptors with a slow dissociation rate, while it shows rapid association and dissociation rates at human NK2 receptors. RO5328673 potently inhibits senktide (HY-P0187)-induced enhancement of spontaneous activity in dopaminergic neurons and reverses senktide-induced changes in motor activity of gerbils. RO5328673 is widely applicable to research related to schizophrenia.

Spantide I, a substance P analog, is a selective NK₁ receptor antagonist, with K_i values of 230 nM and 8150 nM for NK₁ and NK₂ receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.

MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.

SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a K_i 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit.

SDZ NKT 343 is a selective, orally active NK₁ receptor antagonist with an IC₅₀ of 0.62 nM against human NK₁ receptor. SDZ NKT 343 has good analgesic activity.

CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with K_i values of 2.3 nM, 0.54 nM and 0.74 nM, respectively. CS-003 Free base (CS-003) has therapeutic efficacy on respiratory diseases associated with neurokinins.

MDL 105212A is a potent and orally active nonpeptide neurokinin receptor (NK-1/NK-2) tachykinin receptor antagonist. MDL 105212A can be used for the researches of inflammation, immunology and neurological disease, such as asthma.

[D-Trp2,7,9] Substance P is a tachykinin (Neurokinin Receptor) antagonist with K_i values of 1 μM, 1.3 μM, and ~9 μM for NK-1, NK-2,and NK-3 receptor, respectively.

GR 94800 TFA is a potent and selective NK₂ receptor peptide antagonist, with pK_B values of 9.6, 6.4 and 6.0 for NK₂, NK₁ and NK₃ receptors, respectively.

MEN 10207 (acetate) is a selective antagonist of the NK-2 tachykinin receptor. MEN 10207 (acetate) induces tachykinin-induced contractions in rat bladder and guinea pig airways in vivo. MEN 10207 (acetate) inhibits [β-Ala 8 ]-NKA (4-10)-induced enhancement of bladder motility in anesthetized rats and [β-Ala 8 ]-NKA (4-10)-induced enhancement of bronchoconstriction in anesthetized guinea pigs.

SB 414240 is a selective neurokinin-2 receptor (NK-2R) antagonist with K_is of 1 nM and 193 nM for human NK-3R and human NK-2R, respectively. SB 414240 does not bind the human μ-opioid receptor (hMOR). SB 414240 can be used for the study of neurological disease.

UK-224671 is a potent and selective NK2 receptor antagonist. UK-224671 is affected by P-gp efflux and poor intrinsic membrane permeability, resulting in low oral bioavailability.

DNK-333 is a potent and balanced dual NK1 and NK2 receptor antagonist with IC₅₀ values of 4.8 nM and 5.5 nM, respectively. DNK-333 blocks the Neurokinin A (NKA) (HY-P0197)-induced bronchoconstriction in asthma.

TAC 363 is a selective tachykinin NK-2 receptor antagonist. TAC 363 shows a rightward shift in the contractile response curve induced by Neurokinin A (HY-P0197) with a pA₂ of 9.82. TAC 363 has a weak antagonistic effect on NK-1 receptors. TAC 363 can inhibit Neurokinin A-induced bronchoconstriction in guinea pigs with an ED₅₀ of 0.3 mg/kg. TAC 363 can be used for the research of bronchial asthma.

WIN-64821 is a secondary metabolite produced by Aspergillus species, and acts as a Neurokinin Receptor antagonist. The K_i values of WIN-64821 for NK1, NK2 and NK3 receptors are 0.24 (human astrocytoma cells), 0.26 (rat duodenum) and 15.2 (guinea pig forebrain) μM, respectively. WIN-64821 inhibits apamin-induced contraction of rat vas deferens, blocks substance P-induced contraction of guinea pig ileum and Ca²⁺ efflux in human astrocytoma cells. WIN-64821 is applicable to analgesic and anti-inflammatory research.

ZM 253270 is a species-selective non-peptide NK-2 receptor (NK-2R) antagonist. ZM 253270 competitively inhibits the binding of [³H]NKA to native or cloned NK-2R from hamster bladder (K_i=2 nM), but has a weaker inhibitory effect (48-fold) on the binding of [³H]NKA to cloned human NK-2R.