neurokinin receptor

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.

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

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.

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].

Senktide is an agonist of tachykinin NK3 receptor.

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].

NK3R-IN-1 (compound 16x), an orally active imidazolepiperazine derivative, functions as a Neurokinin Receptor NK3R inhibitor and has been demonstrated to reduce blood luteinizing hormone concentrations in an ovariectomy (OVX) model [1].

[D-Pro2] Spantide I TFA is an analog of Spantide I, serving as a selective antagonist of the NK1 receptor [1].

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.

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

(R)-CJ 11974: non-peptide NK1 receptor antagonist, may relieve pain and prevent chemo-induced vomiting.

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.

Neurokinin Receptor (393-407), rat (SPR393–407), a fragment of the rat neurokinin 1 receptor (NK1R), undergoes rapid endocytosis and recycling to the plasma membrane upon substance P (SP) binding and is instrumental in researching neurogenic inflammation [1] [2].

Fosrolapitant is an antagonist of the neurokinin 1 (NK1) receptor.

Casopitant (GW679769) is an orally active neurokinin-1 (NK1) receptor antagonist, researched for its potential use in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).

(1R,2S,3R)-Aprepitant (Compound ent-4) is a competitive antagonist of the human neurokinin-1 (NK-1) receptor. It holds potential for research in the treatment of nausea and vomiting related to cancer or postoperative conditions.

Senktide TFA is a potent and selective neurokinin 3 (NK3) receptor agonist with an EC50 of 0.5-3 nM, while showing significantly weaker activity on NK1 receptors (EC50=35 µM). It is a promising candidate for research in neurological disorders.

LMN-NKA acetate is a modified Neurokinin A (4-10) and selective NK2R (Neurokinin 2 receptor) agonist that induces bladder contraction and urination/defecation in rats, and can be used for studying smooth muscle contraction.

Anthrotainin is a tetracyclic compound that acts as an inhibitor of the binding of P substance (substance P), with an IC50 of 3 μM.

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.

MEN11467 is a novel, orally available, potent and selective peptidomimetic tachykinin NK 1 receptor antagonist for the study of acute colon cancer.

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

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.