[Glp5] Substance P (5-11) is an octapeptide. [Glp5] Substance P (5-11) is one of the main substance P fragments in rat central nervous system (CNS). [Glp5] Substance P (5-11) locally modulates dopamine release in rat striatum[1].
GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pKB of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity[1].
[Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), an analogue of Neurokinin A, is a selective and potent NK2R agonist. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) has prokinetic activity. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) can be used to study the roles of the NK-2 receptor in smooth muscle contraction in numerous tissues[1][2][3].
[DAla4] Substance P (4-11) is an analog of Substance P (Substance P (HY-P0201)) that inhibits the binding of 125I-Bolton Hunter-conjugated Eledoisin (Eledoisin (HY-P0006)) (IC50 of 0.5 μM) and 125I-Bolton Hunter-conjugated Substance P (IC50 of 0.15 μM) to rat brain cortex membranes[1].
Substance P-Gly-Lys-Arg, also known as β-Preprotachykinin (58-71), is an analog of Substance P (Substance P (HY-P0201))[1].
(β-Ala8)-Neurokinin A (4-10), a neuropeptide, is a potent and selective NK-2 tachykinin receptor (Neurokinin Receptor) agonist[1].
MDL 29913, a cyclic pseudopeptide, is a competitive NK2 tachykinin receptor selective antagonist, with a pA2 of 8.66[1].
Substance P (alligator), a Substance P (Substance P (HY-P0201)) extracted from alligator, is a neuropeptide. The primary structure of Substance P (alligator) is: Arg-Pro-Arg-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2[1].
Elinzanetant is a neurokinin receptors antagonist used for the research of Schizophrenia[1].
GR 94800 is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively[1][2].
[Pro9]-Substance P is a potent, reversible and selective agonist of NK-1 tachykinin receptors with an EC50 of 0.93 nM[1].
Neurokinin B belongs to the tachykinin family of peptides. Neurokinin B binds a family of GPCRs—including neurokinin receptor 1 (NK1R), NK2R, and NK3R-to mediate their biological effect.
Substance P (5-11), the C-terminal heptapeptide of Substance P (Substance P (HY-P0201)), is a neuropeptide. Substance P (5-11) binds to NK-1 tachykinin receptor[1].
Fosaprepitant (L-758298) is a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.IC50 Value:Target: NK1 receptorin vitro: Fosaprepitant (also known as MK-0517 and L-758,298) is a water-soluble phosphoryl prodrug for aprepitant, which, when administered intravenously, is converted to aprepitant within 30 min of intravenous administration via the action of ubiquitous phosphatases. Owing to the rapid conversion offosaprepitant to the active form (aprepitant), fosaprepitant 115 mg provided the same aprepitant exposure in terms of AUC as aprepitant 12 mg orally, and fosaprepitant is expected to provide a correspondingly similar antiemetic effect as aprepitant [1]. in vivo: Fosaprepitant is well tolerated with mild to moderate venous irritation being the only additional toxicity to those seen with oral aprepitant, and that is a function of dose, concentration, and infusion rate [2]. Patients receiving cisplatin ≥ 70 mg/m(2) for the first time received ondansetron and dexamethasone with a standard aprepitant regimen (125 mg on day 1, 80 mg on day 2, 80 mg on day 3) or a single-dose fosaprepitant regimen (150 mg on day 1) [3]. Single-dose fosaprepitant used in combination with granisetron and dexamethasone was well-tolerated and effective in preventing chemotherapy-induced nausea and vomiting in patients receiving highly emetogenic cancer chemotherapy, including high-dose cisplatin [4].
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 Ki of 0.26 nM[1].
[Sar9,Met(O2)11]-Substance P is a tachykinin NK1 receptor selective agonist.
Tachykinin angatonist 1 is a neurokinin receptor antagonist extracted from patent US5968923, compound example 32.
QWF Peptide (Compound 4a) is a substance P antagonist with an IC50 of 0.09 μM. QWF Peptide antagonizes the SP-induced contraction of isolated guinea pig trachea strips with an IC50 of 4.7 μM[1].
CP-96,345 is a specific, highly potent, and orally active tachykinin and substance P receptor non-peptide inhibitor. CP-96,345 prevents the drop in blood pressure evoked by substance P and neurokinin A. CP-96,345 can be used for researching neurogenic inflammation[1].
Substance P (6-11) is the C-terminal hexapeptideamide of Substance P (Substance P (HY-P0201)). Substance P (6-11) binds to NK-1 tachykinin receptor. Substance P (6-11) shows depolarization of motoneurons and a hypotensive effect[1][2].
Neurokinin A acts via neurokinin 2 (NK-2) receptor.
Imnopitant dihydrochloride is a neurokinin NK1 receptor antagonist[1].
[Nle11]-Substance P is a substance P analog that avoids methionine oxidation problems.
[MePhe7]-Neurokinin B is an neurokinin NK-3 receptor (NK3R) agonist with an IC50 value of 3 nM. [MePhe7]-Neurokinin B is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R)[1].
Spantide II, an undecapeptide substance P (SP) analog, is a potent neurokinin-1 receptor (NK-1R) antagonist. Spantide II binds with NK-1R and blocks proinflammatory activities associated with SP. Spantide II can be used in the research of inflammatory skin disorders, such as psoriasis and contact dermatitis[1][2][3].
Imnopitant is a NK1 receptor antagonist (WO2020132716, compound 1) [1].
[Glp5,Sar9] Substance P (5-11) is an analogue of Substance P (HY-P0201)[1].
GR203040 is an orally active NK1 receptor antagonist with a pKi of 10.3. GR203040 shows potent antiemetic activity[1].
SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 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[1][2].
(D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P is a neuropeptide Substance P (HY-P0201) antagonist[1].