Neurokinin receptor

Neurokinin B acetate(86933-75-7 free base) is the acetate form of Neurokinin B, which belongs to the tachykinin family. Neurokinin binds to neurokinin receptor 1 (NK1R), nk2r and NK3R, and mediates its biological effects.

Substance P (Neurokinin P) (SP) is an undecapeptide (a peptide composed of a chain of 11 amino acid residues) member of the tachykinin neuropeptide family.

Fezolinetant (ESN-364) is a neurokinin-3 receptor antagonist that is being investigated for menopausal hot flashes.

Neurokinin A (NKA), formerly known as Substance K, is a neurologically active peptide translated from the pre-protachykinin gene.

WIN 51,708 is a neurokinin receptor (NK1) antagonist.

Elinzanetant is a dual antagonist of neurokinin (NK) receptors 1 and 3 and modulates reproductive hormone secretion.

SB 218795 is an effective and selective antagonist of NK3 with a Ki 13 nM for hNK3 which is about 90-fold and 7000-fold selectivity over hNK2 and hNK1.

Befetupitant (Ro67-5930) is a potent and selective tachykinin 1 receptor (NK1R) antagonist for the study of corneal neovascularization.

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.

Netupitant (CID 6451149) is a specific neurokinin 1 (NK1) receptor antagonist (Ki: 0.95 nM).

Pavinetant (MLE-4901) is an orally available neurokinin-3 receptor (NK3R) antagonist used to improve menopausal symptoms.

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.

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.

Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).

Highy selective and potent NK2 receptor agonist (IC50 = 6.1 nM). Induces contraction of the rat fundus and bladder (EC50 values are 117 and 10 nM respectively).

Maropitant citrate is a synthetic neurokinin-1 receptor antagonist and substance P inhibitor, used for controlling vomiting in cats and dogs.

Tradipitant (VLY-686) is an antagonist of neurokinin-1.

QWF acetate is a Substance P antagonist that specifically inhibits the binding of Substance P to its receptor (NK1) with an IC50 of 0.09 Μm; it can also inhibit the activation of Mas-related G-protein-coupled receptor X2 (MRGPRX2), which inhibits degranulation of mast cells.QWF acetate is used as a polypeptide in pain, inflammation and allergic reactions, QWF acetate has important applications as a peptide in the study of pain, inflammation and allergic reactions.

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.

Senktide is an agonist of tachykinin NK3 receptor.

Substance P (7-11) (Substance P 7-11(TFA)) is a C-terminal fragment of Substance P .

SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4 nM).

NKP608 is a selective and highly effective neurokinin-1 (NK-1) receptor antagonist with anticancer and antianxiety activities, inhibiting the proliferation of human colorectal cancer cells through the Wnt signaling pathway.

Neurokinin A(4-10) TFA(97559-35-8 free base) is a tachykinin NK2 receptor agonist[1].

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.

Ezlopitant (CJ-11974) is a small molecule neurokinin-1-receptor (NK1) antagonist used to treat nausea, vomiting and pain.

Fosaprepitant dimeglumine (MK-0517) is the dimeglumine salt form of fosaprepitant, a water-soluble, N-phosphorylated prodrug of aprepitant with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent selectively binds to human substance P neurokinin 1 (NK1) receptors in the central nervous system (CNS), inhibiting receptor binding of endogenous substance P and preventing substance P-induced emesis.

Vapreotide acetate (BMY-41606 acetate) is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM).

[Sar9,Met(O2)11]-Substance P (NA) is an NK1 receptor agonist.

Substance P(1-7) TFA is a fragment of neuropeptide P (SP) with anti-nociceptive activity. It prevents morphine-induced spontaneous pain behavior through the spinal NMDA-NO cascade, and can be used in research on neurological diseases.

Eledoisin Related Peptide 2TFA (Eledoisin Related Peptide 2TFA (2990-43-4(free base))) is a tachykinin receptor ligand.

Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting, and orally active neurokinin 1 (NK1) receptor antagonist with a K_i of 0.66 nM, which does not interact with CYP3A4 and demonstrates potent centrally-mediated anti-emetic activity in both acute and delayed ferret emesis models [1] [2].

N-Acetyl-L-tryptophan (N-acetyltryptophan) is an inhibitor of neurokinin 1 receptor (NK1-receptor, NK1R).

Eprazinone dihydrochloride (NSC 317935) is a mucolytic with antitussive and mucolytic effect.

Vofopitant dihydrochloride (GR 205171A) is an orally available, selective tachykinin NK1 receptor antagonist that inhibits [3H]SP binding to NK1 with pKi values of 9.5 and 10.6, respectively. It is a potential compound for the treatment of pathological vomiting.

Burapitant (SSR 240600) is a novel non-peptide tachykinin neurokinin 1 (NK) receptor antagonist with anti-coke oven and antidepressant activity.

R 396 acetate is an NK-2 Tachykinin Receptor Antagonist.

L-732138 is a potent and competitive antagonist of neurokinin-1 (NK-1) receptor(IC50 : 2.3 nM)

Spantide acetate is a selective antagonist of NK1 receptor with Kis of 230 nM and 8150 nM for NK1 and NK2.

[Sar9,Met(O2)11]-Substance P acetate is a tachykinin NK1 receptor selective agonist. [Sar9,Met(O2)11]-Substance P acetate is a selective tachykinin NK1 receptor agonist.[Sar9,Met(O2)11]-Substance P acetate and septide (10-100 pmol per rat, i.c.v.) are equipotent in increasing mean arterial blood pressure (MAP) and heart rate (HR), yet they have dissimilar time-course. Both agonists increase dose-dependently face washing and sniffing while [Sar9,Met(O2)11]-Substance P acetate is the sole to produce grooming.

C14TKL-1 acetate is a NK1 receptor agonist.

MEN 10207 acetate is a selective antagonist for NK-2 tachykinin receptor.

Hemokinin 1 (mouse) acetate is a selective excitogen 1 receptor agonist with a Ki value of 0.175 nM for the human NK1 receptor and 560 nM for the human NK2 receptor.

Potent and selective tachykinin NK1 receptor agonist (EC50 = 2 nM in guinea pig vas deferens).

GR 94800 acetate is a potent and selective neurokinin 2(NK-2) antagonist.

[Sar9]-Substance P acetate is one of NK-1 receptor agonist. The action of SP on progesterone metabolism was mimicked by the rNK1-specific agonist [Sar-9,Met(O2)11]-SP.

Physalaemin acetate is a non-mammalian tachykinin with high affinity when binding selectively to neurokinin-1 (NK1) receptor.