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NK3 Receptor Antagonist

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By Targets:	Neurokinin Receptor (34) Apoptosis (1) Bcl-2 Family (1) Cadherin (1) Calcium Channel (1) Caspase (1) Cyclin G-associated Kinase (GAK) (1) Endogenous Metabolite (1) Neurotensin Receptor (1) Reference Standards (3) VEGFR (1) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (5) Cardiovascular Disease (1) Endocrinology (9) Infection (1) Inflammation/Immunology (5) Metabolic Disease (1) Neurological Disease (30)

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Targets Recommended: Neurokinin Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-19632

Fezolinetant 5 Publications Verification ESN-364	Neurokinin Receptor	Endocrinology
Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.

HY-109171

Elinzanetant NT-814; BAY3427080	Neurokinin Receptor	Cardiovascular Disease Neurological Disease
Elinzanetant is an orally active and selective NK-1 and *NK-3* receptor antagonist. Elinzanetant alleviates menopause-associated vasomotor symptoms, including hot flashes and night sweats. Elinzanetant reduces estradiol and progesterone levels. Elinzanetant can be used for the research of moderate to severe vasomotor and sleep disorders associated with menopause .

HY-15722

SB-222200 Maximum Cited Publications 6 Publications Verification	Neurokinin Receptor	Neurological Disease Endocrinology
SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant **NK-3 receptor** antagonist. SB-222200 is developed for central nervous system (CNS) disorders .

HY-14432

Pavinetant 3 Publications Verification MLE-4901; AZD2624; AZD4901	Neurokinin Receptor	Neurological Disease Endocrinology
Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.

HY-14552

Talnetant 3 Publications Verification SB 223412	Neurokinin Receptor	Neurological Disease Endocrinology
Talnetant (SB 223412) is a selective, competitive, brain-permeable *NK3* receptor antagonist with a K_i of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies .

HY-101249

L-732138	Neurokinin Receptor	Neurological Disease Cancer
L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC₅₀ of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action .

HY-14551

Osanetant SR142801	Neurokinin Receptor	Neurological Disease
Osanetant (SR142801) is a selective **NK3 receptor** antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia .

HY-P1192

GR-73632	Neurokinin Receptor	Neurological Disease
GR-73632 is a tachykinin NK1 receptor agonist. GR-73632 activates spinal NK1 receptors to induce scratching, biting and licking behaviors. GR-73632 activates peripheral NK1 receptors to trigger lacrimation in guinea pigs, and activates central NK1 receptors to induce repetitive hind paw tapping behavior in gerbils. GR-73632 is applicable to research related to pruritus .

HY-107691

GR 159897	Neurokinin Receptor	Neurological Disease Endocrinology Cancer
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 .

HY-133206A

Fosnetupitant chloride monohydrochloride 1 Publications Verification Pronetupitant chloride monohydrochloride	Neurokinin Receptor	Cancer
Fosnetupitant chloride monohydrochloride (Pronetupitant chloride monohydrochloride) is an NK1 antagonist with pK_i values of 9.5, 6.1 for human NK1 and NK3 receptor, respectively. Fosnetupitant chloride monohydrochloride is a methylene phosphate prodrug of Netupitant .

HY-117380

SB 235375	Neurokinin Receptor	Neurological Disease
SB 235375 is a potent and selective antagonist of the human neurokinin-3 (hNK-3) receptor designed by optimizing the structure of 2-phenyl-4-quinolinecarboxylic acid amide. SB 235375 displays high affinity for the hNK-3 receptor, with significantly higher binding affinities than hNK-2 and hNK-1 receptors. In vitro studies demonstrated its ability to block NK-3 receptor-mediated contraction and calcium mobilization, while in vivo, SB 223412 demonstrated oral and intravenous activity against NK-3 receptor-driven responses in animal models .

HY-18006

NKP608 1 Publications Verification	Neurokinin Receptor Wnt Bcl-2 Family β-catenin Cyclin G-associated Kinase (GAK) VEGFR Caspase Cadherin Apoptosis	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
NKP608 is a non-peptidic derivative of 4-aminopiperidine, a highly selective, orally active, neurokinin-1 (NK₁) receptor antagonist with IC₅₀ of 2.6 nM. NKP608 is active both in vitro and in vivo, showing extremely low affinity for NK₂, NK₃ receptors. NKP608 exerts its effects by blocking the NK₁ receptor, regulate cell proliferation and apoptosis, affect neurotransmitter functions and gastric mucosal repair mechanisms, and suppress the Wnt/β-catenin pathway in antitumor research. NKP608 is applicable to research related to various diseases, including cough, anxiety disorders, depression, gastric mucosal injury, and colorectal cancer .

HY-P3854

GR 83074	Neurokinin Receptor	Neurological Disease
GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pK_B of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity .

HY-151413

MEN 10207 1 Publications Verification	Neurokinin Receptor	Neurological Disease
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.

HY-P1277

GR 94800	Neurokinin Receptor	Neurological Disease
GR 94800 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 .

HY-116822

SSR 146977	Neurokinin Receptor	Neurological Disease
SSR 146977 is a potent and selective antagonist of the tachykinin **NK3 receptor*. SSR 146977 inhibits the binding of radioactive neurokinin B to NK3* receptors in Chinese hamster ovary cells, with a K_i of 0.26 nM .

HY-14551B

(S)-Osanetant (S)-SR142801	Neurotensin Receptor	Neurological Disease
(S)-Osanetant is the S-enantiomer of Osanetant. Osanetant (SR142801) is a selective **NK3 receptor** antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia .

HY-14552A

Talnetant hydrochloride SB 223412 hydrochloride; SB 223412-A	Neurokinin Receptor	Neurological Disease Endocrinology
Talnetant (SB 223412) hydrochloride is a selective, competitive, brain-permeable *NK3* receptor antagonist with a K_i of 1.4 nM in hNK-3-CHO cells. Talnetant hydrochloride is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant hydrochloride can be used in schizophrenia-related studies .

HY-121164

GSK172981	Neurokinin Receptor	Neurological Disease
GSK172981 is a brain-penetrant tachykinin NK3 receptor antagonist with pK_i values of 7.7 and 7.8 for human and native guinea pig NK3 receptors, respectively. GSK172981 can be used for the study of schizophrenia .

HY-14551C

Osanetant monohydrochloride SR142801 monohydrochloride	Neurokinin Receptor	Neurological Disease
Osanetant (SR142801) monohydrochloride is a selective **NK3 receptor** antagonist. Osanetant monohydrochloride produces anxiolytic- and antidepressant-like effects .

HY-107692

SB 218795	Neurokinin Receptor	Neurological Disease
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 .

HY-107693

SSR 146977 hydrochloride	Neurokinin Receptor	Neurological Disease Inflammation/Immunology
SSR 146977 hydrochloride is a potent and selective antagonist of the tachykinin *NK₃* receptor. SSR 146977 hydrochloride can be used in the study of psychiatric disorders and airway inflammation .

HY-P3802

[D-Trp2,7,9] Substance P	Neurokinin Receptor	Neurological Disease
[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 .

HY-116958

SCH 206272	Neurokinin Receptor	Inflammation/Immunology
SCH 206272 is a selective antagonist of the tachykinin (NK) receptor. SCH 206272 inhibits binding at human tachykinin NK(1), NK(2), and NK(3) receptors (K_i = 1.3, 0.4, and 0.3 nM, respectively). SCH 206272 has an orally active .

HY-P1277A

GR 94800 TFA	Neurokinin Receptor	Neurological Disease
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 .

HY-116268

GSK256471	Neurokinin Receptor	Neurological Disease
GSK256471 is a non-peptide tachykinin **NK3 receptor** antagonist with a pK_i of 8.9 for the human recombinant NK3 receptor and 8.4 for the guinea pig native receptor. GSK256471 exhibits >100-fold selectivity for NK1 (pK_i = 5.2) and NK2 (pK_i = 7.3) receptors. GSK256471 noncompetitively inhibits neurokinin B (NKB) (HY-P0242)-induced inositol phosphate accumulation, and this inhibition is irreversible. GSK256471 inhibits wet dog shaking behavior and suppresses dopamine release. GSK256471 could be used to study schizophrenia .

HY-19633

CS-003 Free base	Neurokinin Receptor	Infection Endocrinology
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.

HY-182423

RO5328673	Neurokinin Receptor	Neurological Disease
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 .

HY-120167

YM-44778	Neurokinin Receptor	Neurological Disease Inflammation/Immunology
YM-44778 is a neurokinin receptor antagonist. The _pK_i values for NK1, NK2 and NK3 are 8.08, 8.55 and 8.24, respectively. YM-44778 inhibits the increase of bladder pressure induced by substance [Sar9,Met(O2)11] -P (HY-P1012) in anestheticized rats .

HY-107692R

SB 218795 (Standard)	Reference Standards Neurokinin Receptor	Neurological Disease
SB 218795 (Standard) is the analytical standard of SB 218795 (HY-107692). This product is intended for research and analytical applications. 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 .

HY-122286

SB 414240	Neurokinin Receptor	Neurological Disease
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 .

HY-14432R

Pavinetant (Standard) MLE-4901 (Standard); AZD2624 (Standard); AZD4901 (Standard)	Neurokinin Receptor Reference Standards	Neurological Disease Endocrinology
Pavinetant (Standard) is the analytical standard of Pavinetant. This product is intended for research and analytical applications. Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.

HY-101249R

L-732138 (Standard)	Neurokinin Receptor Reference Standards	Neurological Disease Cancer
L-732138 (Standard) is the analytical standard of L-732138 (HY-101249). This product is intended for research and analytical applications. L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action .

HY-N9554

WIN-64821	Neurokinin Receptor Endogenous Metabolite Calcium Channel	Neurological Disease Inflammation/Immunology
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 Ca ²⁺ efflux in human astrocytoma cells. WIN-64821 is applicable to analgesic and anti-inflammatory research .

HY-181682

NK3R antagonist-1	Neurokinin Receptor	Endocrinology
NK3R antagonist-1 is an orally active neurokinin-3 receptor (NK3R) antagonist with an IC₅₀ of 53.61 nM. NK3R antagonist-1 reduces plasma luteinizing hormone (LH) levels in ovariectomized rat models. NK3R antagonist-1 is applicable to research related to menopausal hot flushes .

Cat. No.	Product Name	Target	Research Area

HY-P1192

GR-73632	Neurokinin Receptor	Neurological Disease
GR-73632 is a tachykinin NK1 receptor agonist. GR-73632 activates spinal NK1 receptors to induce scratching, biting and licking behaviors. GR-73632 activates peripheral NK1 receptors to trigger lacrimation in guinea pigs, and activates central NK1 receptors to induce repetitive hind paw tapping behavior in gerbils. GR-73632 is applicable to research related to pruritus .

HY-P3854

GR 83074	Neurokinin Receptor	Neurological Disease
GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pK_B of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity .

HY-151413

MEN 10207 1 Publications Verification	Neurokinin Receptor	Neurological Disease
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.

HY-P1277

GR 94800	Neurokinin Receptor	Neurological Disease
GR 94800 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 .

HY-P3802

[D-Trp2,7,9] Substance P	Neurokinin Receptor	Neurological Disease
[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 .

HY-P1277A

GR 94800 TFA	Neurokinin Receptor	Neurological Disease
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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N9554

WIN-64821	Structural Classification Microorganisms Ketones, Aldehydes, Acids Source Classification	Neurokinin Receptor Endogenous Metabolite Calcium Channel
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 Ca ²⁺ efflux in human astrocytoma cells. WIN-64821 is applicable to analgesic and anti-inflammatory research .

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NK3 Receptor Antagonist

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