Neurokinin receptor

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.

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

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.

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.

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.

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

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.

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

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.

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

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).

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

Senktide is an agonist of tachykinin NK3 receptor.

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.

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.

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.

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

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

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

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

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

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].

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

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

[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.

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

C14TKL-1 acetate is a NK1 receptor agonist.

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

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

[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.

Men 10376 TFA(135306-85-3,free) (Neurokinin-2 receptor antagonist TFA) is an effective and selective tachykinin nk-2 receptor antagonist with a K I value of 4.4 M for the nk-2 receptor in the small intestine of rats.

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

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

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

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

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.

(R)-CJ 11974 is a novel non-peptide neurokinin NK1 substance P receptor antagonist with potential analgesic activity that can be used to study chemotherapy-induced vomiting.

Maropitant is a selective neurokinin (NK1) receptor antagonist.

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

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.

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

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

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

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.