nk3 receptor

AMPA receptor antagonist-3 is an AMPA receptor antagonist.

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

GLP-1 receptor agonist 3 is a GLP-1 receptor agonist,Example 4A-1, has EC50s of 1.1 nM and 13 nM in Clone H6 and Clone C6 cell lines assay, respectively.

Estrogen receptor antagonist 3 is a potent degradation agent of the estrogen receptor (ER). Estrogen signaling systems regulate cell growth, differentiation, and apoptosis, and estrogen receptor antagonist 4 has shown potential for cancer research.

Mu opioid receptor antagonist 3 (compound 26) is a potent and selective MOR antagonist with the ability to penetrate the blood-brain barrier (Ki: 0.24 nM, EC50: 0.54 nM). This compound can be used to study opioid use disorder (OUD).

Adenosine receptor antagonist 3 has the potential for cancer disease research which is a potent adenosine receptor antagonist [1].

TGR5 Receptor Agonist 3 is a G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist soft drug compound that decreases gallbladder filling, exhibits good gallbladder safety, and is able to act on hTGR5 (EC50: 16.4 nM) and mTGR5 (EC50: 209 nM).

Androgen receptor antagonist 3 (Compound C18) exhibits anticancer activity as an antagonist of the androgen receptor (AR) with an IC50 value of 2.4 μM [1].

Compound 5e, a GPR34 receptor antagonist, exhibits selective inhibition of lysophosphatidylserine-induced ERK1 2 phosphorylation in a dose-dependent manner, demonstrating an IC50 value of 0.680 μM without significant cytotoxicity. Additionally, it displays antisensory activity in a mouse neuropathic pain model [1].

NMDA receptor modulator 3 (Compound 99) is a potent NMDA receptor modulator useful in neurological disorder research [1].

5-HT2A receptor agonist-3 represents the highest selectivity for the human 5-HT2A receptor currently identified, exhibiting a K i of 2.5 nM. It also demonstrates a remarkable 124-fold selectivity over its structurally analogous 5-HT2C receptor [1].

EP4 receptor antagonist 3 is a highly potent and specific inhibitor of the EP4 receptor, intended for research purposes in studying EP4 receptor-mediated diseases, including acute and chronic pain, osteoarthritis, rheumatoid arthritis, and cancer.

ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist with an IC50 of 0.26 nM, utilized for pulmonary arterial hypertension (PAH) research. This compound demonstrates efficacy in mitigating monocrotaline-induced PAH in a rat model [1].

Glucagon receptor antagonist -3 is a highly effective glucagon receptor antagonist.

TFRGAP-amide, human PAR-3-derived tethered ligand sequence which does not activate PAR-3 but rather activates PAR-1 and PAR-2, either in Jurkat or in other PAR-expressing cells.

P2X7 receptor antagonist-3 is a potent inhibitor of the P2X7 receptor, with IC50 values of 4.2 nM in humans and 6.8 nM in rats, demonstrating its high efficacy across species.

Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA, is a peptide that acts as an agonist for the proteinase-activated receptor (PAR-3) [1].

RXFP1 receptor agonist-3 (Example 223) is an RXFP1 receptor agonist that inhibits cyclic AMP (cAMP) production in HEK293 cells stably expressing human RXFP1, with an EC50 of 2 nM [1].

NMDA receptor antagonist-3 is a NMDA receptor antagonist with a significan recovery rate (40.0%, at 100 μM) and safe toxicological characteristics in SH-SY5Y and human adipose mesenchymal stem cells.

Androgen Receptor Degrader-3 (ARD-3) is a compound that inhibits androgen receptor signaling and promotes the degradation of the receptor, with potential applications in prostate cancer research [1].

Orexin receptor antagonist 3 (example 216) functions as an orexin receptor antagonist.

A2A receptor antagonist 3 (Example 92) is an adenosine A2A receptor antagonist (Ki: 0.4 nM) and a receptor (Ki: 1467 nM).

Protease-Activated Receptor-1 antagonist 3 is a potent antagonist of Protease-Activated Receptor-1 (IC50: 7 nM) and exhibits binding affinity to hERG K+ channels (IC50: 9 μM).

GP 2A is a selective agonist of CB2 receptor.

Compound 20, identified as μ opioid receptor agonist 3, is a potent µOR agonist that exhibits an EC50 value of 0.87 nM. It holds promise for research into pain management and neuropsychiatric disorders [1].

APJ receptor agonist 3 is a highly effective, orally administrable APJ receptor agonist, with a potent EC50 value of 0.027 nM.

Scyliorhinin II acetate is a selective agonist of the neurokinin-3 (NK3) receptor (Ki = 2.5 nM) in rat cerebral cortex.

Hemokinin 1 (human) acetate is an endogenous substance P homolog that is a selective agonist at the tachykinin NK1 receptor (IC50 values are 1.8, 370 and 480 nM for NK1, NK3 and NK2 receptors respectively). Has proliferative and antiapoptotic actions on B

Talnetant (SB 223412) is a selective, competitive NK3 receptor antagonist that penetrates the brain and modulates mesolimbic and mesocortical dopaminergic neurotransmission.

NK3 receptor antagonist

Fosnetupitant chloride monohydrochloride (Pro-netupitant chloride monohydrochloride) is a selective NK1 antagonist exhibiting high affinity for the human NK1 receptor with a pK i value of 9.5, and a lower affinity for the NK3 receptor with a pK i of 6.1. It serves as a methylene phosphate prodrug of Netupitant [1].

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

Talnetant (SB 223412) hydrochloride is a selective NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. It is 100 times more selective for the hNK-3 receptor than the hNK-2 receptor and shows no affinity for hNK-1 at a concentration of 100 μM.

Hemokinin 1, human TFA acts as a selective full agonist at the tachykinin neurokinin 1 (NK1) receptor, while also being a full agonist at NK2 and NK3 receptors. It is capable of inducing opioid-independent analgesia [1] [2].

Potent and selective tachykinin NK2 receptor agonist (EC50 = 3.7 nM in rat colon). Displays > 1000- and > 300-fold selectivity over NK1 and NK3 receptors respectively. Active in vivo.

Scyliorhinin II, a cyclic Tachykinin peptide, is a potent NK3 receptor agonist.

Osanetant produces anxiolytic- and antidepressant-like effects. Osanetant is a selective NK3 receptor antagonist. It is researched for schizophrenia.

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......

GSK172981 is a non-peptide tachykinin NK3 receptor antagonist with a high affinity for the recombinant human (PK (I) value 7.7) and native guinea pig (PK (I) value 7.8) tachykinin NK3 receptor. In vitro, the functional evaluation showed that GSK172981 was

Endogenous substance P homolog that is a selective agonist at the tachykinin NK1 receptor (IC50 values are 1.8, 370 and 480 nM for NK1, NK3 and NK2 receptors respectively). Has proliferative and antiapoptotic actions on B-cells in vitro and is antihyperte

GR 94800 TFA is a potent, selective antagonist of the NK 2 receptor peptide, demonstrating pK B values of 9.6 for NK 2, 6.4 for NK 1, and 6.0 for NK 3 receptors, respectively [1] [2].

Senktide acetate (Senktide acetate(106128-89-6 free base)) is a selective tachykinin NK3 receptor agonist that promotes the consolidation or expression of ELM for the study of Alzheimer's disease.

(S)-Osanetant, the S-enantiomer of Osanetant (SR142801), is a selective NK3 receptor antagonist known for its anxiolytic- and antidepressant-like effects. It is currently under investigation for potential use in treating schizophrenia [1].

GR 64349 is a potent and highly selective NK2 receptor peptide antagonist with an EC50 of 3.7 nM in rat colon, exhibiting over 1000-fold selectivity against NK1 receptors and over 300-fold selectivity against NK3 receptors, ensuring targeted action [1] [2].

RO4583298 is a highly potent dual NK1/NK3 receptor antagonist with in vivo activity.

Senktide is an agonist of tachykinin NK3 receptor.