neurokinin receptors

Saredutant (SR 48968) is a selective neurokinin-2 (NK2) receptor antagonist that inhibits the action of neurokinin A by blocking the NK2 receptor, thereby exerting antidepressant and anxiolytic effects.

gamma-preprotachykinin amide (72-92) acetate is a 21 amino acid peptide belonging to the tachykinin (TK) family and including neurokinin A (NKA) in its C-terminal sequence. gamma-preprotachykinin amide (72-92) acetate possesses higher affinity than NKA for central NK-2 receptors; it shows lower affinity for NK-1 receptors, however, it potently stimulates salivary secretion, which is mediated by NK-1 receptor activation.

Tachykinin antagonist 1 is an antagonist of neurokinin receptors.

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

SSR-241586 is a neurokinin receptors antagonist,and is shown to be active in the treatment of depression, schizophrenia, urinary trouble, emesis, and irritable bowel syndrome (IBS).

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.

DNK 333 is a dual antagonist targeting the neurokinin NK1 NK2 receptors.

GSK256471 is a potent selective NK(3) antagonist that shows a high affinity for recombinant human (PK (I) value 8.9) and native guinea pig (PK (I) value 8.4) tachykinin NK(3) receptors. In vitro functional assessment showed that GSK256471 reduced the E(Ma

Benzomalvin B is a fungal metabolite originally isolated from Penicillium. It acts as an antagonist of neurokinin-1 (NK1) receptors, inhibiting binding of substance P by 24% in vitro when used at a concentration of 100 μg/ml.

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

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......

Acetylaszonalenin is a fungal metabolite that has been found in A. flavipes.1 It acts as an antagonist of neurokinin-1 (NK1) receptors, inhibiting binding of substance P with a Ki value of 170 μM.

WIN 66306 is a cyclic heptapeptide antagonist of neurokinin-1 (NK1) and NK2 receptors originally isolated from A. flavipes. It binds to NK1 and NK2 receptors and inhibits contractions induced by substance P in isolated guinea pig ileum in a concentration-dependent manner.

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].

[D-Trp2,7,9] Substance P is a tachykinin (Neurokinin Receptor) antagonist with inhibitory affinities (K_i values) of 1 μM for NK-1, 1.3 μM for NK-2, and approximately 9 μM for NK-3 receptors [1].

Substance P(1-4) acts as a potent antagonist of neurokinin receptors (NK-R) and regulates normal hematopoiesis, additionally inhibiting the formation of endogenous erythroid colonies (EEC) [1].

Fosaprepitant-d4 Dimeglumine is a deuterated compound of Fosaprepitant Dimeglumine. Fosaprepitant Dimeglumine has a CAS number of 265121-04-8. Fosaprepitant Dimeglumine is the dimeglumine salt form of fosaprepitant, the water-soluble, N-phosphorylated prodrug of aprepitant, with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent binds selectively to the human substance P neurokinin 1 (NK1) receptors in the central nervous system (CNS). This inhibits receptor binding of the endogenous substance P and prevents substance P-induced emesis.

Neurokinin B TFA, a member of the tachykinin family, binds to a series of GPCRs, including neurokinin receptors 1 (NK1R), NK2R, and NK3R, to modulate their biological effects.

Scyliorhinin I is an agonist for both neurokinin-1 (NK-1) and neurokinin-2 (NK-2) receptors, exhibiting a Ki value of 0.9 nM at rat submandibular gland NK-1 receptors and 2 nM at hamster bladder NK-2 receptors. Additionally, it possesses the capability to contract the longitudinal muscle of the guinea pig ileum.