| Name | neurokinin 1 receptors |
|---|---|
| Synonyms | NK 1 receptor; NK 1R; NK1R; NKIR; Neurokinin 1 receptor; SPR; Substance P Receptor; TAC1R… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 15982585 | Gao M, Mock BH, Hutchins GD, Zheng QH: Synthesis and initial PET imaging of new potential NK1 receptor radioligands 1-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-4-[11C] methyl-pip erazine and {4-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-piperazine-1-yl} - [11C] methyl ester. Nucl Med Biol. 2005 Jul;32(5):543-52. The NK (1) receptor radioligands 1-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-4-[(11) C] methyl-p iperazine ([(11) C] BMP, [(11) C]) and {4-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-piperazine-1-yl} - [(11) C] methyl ester ([(11) C] BME, [(11) C]) were synthesized for evaluation as new potential PET imaging agents for brain NK (1) receptors. |
31(0,1,1,1) | Details |
| 15145080 | Johnson PJ, Bornstein JC: Neurokinin-1 and -3 receptor blockade inhibits slow excitatory synaptic transmission in myenteric neurons and reveals slow inhibitory input. Neuroscience. 2004;126(1):137-47. They were abolished by the 5-hydroxytryptamine (1A) receptor antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl]-piperazine (NAN-190), but unaffected by phentolamine, an alpha-adrenoceptor antagonist. This study investigated a similar role for neurokinin-1 receptors (NK (1) R) and compared the effect of selective receptor antagonists on non-cholinergic slow excitatory post-synaptic potentials (EPSPs) recorded in myenteric AH neurons of the guinea-pig ileum. |
1(0,0,0,1) | Details |
| 19388677 | Di Fabio R, Griffante C, Alvaro G, Pentassuglia G, Pizzi DA, Donati D, Rossi T, Guercio G, Mattioli M, Cimarosti Z, Marchioro C, Provera S, Zonzini L, Montanari D, Melotto S, Gerrard PA, Trist DG, Ratti E, Corsi M: Discovery process and pharmacological characterization of 2-(S)-(4--2-methylphenyl) piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl) ethyl] methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist. J Med Chem. 2009 May 28;52(10):3238-47. Among the compounds synthesized, 2-(S)-(4--2-methylphenyl) piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl) ethyl] methylamide (vestipitant) was identified as one of the most in vitro potent and selective NK (1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. |
32(0,1,1,2) | Details |
| 16289817 | van den Hoogenband A, van Maarseveen JH, McCreary AC, Mulder AT, van Scharrenburg GJ, van Stuivenberg HH, Zethof TJ, Zijta B, Iwema Bakker WI: Piperazinyl oxime ethers as NK-1 receptor antagonists. . Bioorg Med Chem Lett. 2006 Feb 15;16(4):1045-8. Epub 2005 Nov 11. The new compounds are based on piperazine 2 and contain an oxime ether functionality. |
3(0,0,0,3) | Details |
| 19420128 | Pellegatti M, Bordini E, Fizzotti P, Roberts A, Johnson BM: Disposition and metabolism of radiolabeled casopitant in humans. Drug Metab Dispos. 2009 Aug;37(8):1635-45. Epub 2009 May 6. In addition, many other metabolites were identified in plasma and excreta: the principal route of metabolism included multiple oxidations, loss of the N-acetyl group, modifications or loss of the piperazine group, and cleavage of the molecule. Casopitant [1-piperidinecarboxamide,4-(4-acetyl-1-piperazinyl)-N-((1R)-1-(3,5-bis (tri fluoromethyl) phenyl)-ethyl)-2-(4--2-methylphenyl)-N-methyl-(2R,4S)-( GW679769)] is a novel neurokinin-1 receptor antagonist being developed for the prevention of chemotherapy-induced and postoperative nausea and vomiting. |
1(0,0,0,1) | Details |
| 12372532 | Ryckmans T, Berton O, Grimee R, Kogej T, Lamberty Y, Pasau P, Talaga P, Genicot C: Dual NK (1) antagonists-- reuptake inhibitors as potential antidepressants. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3195-8. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives.. Compound 7u was shown to be active in animal models of reuptake inhibition and central NK (1) receptor blockade, and was demonstrated to be orally active in an integrated model sensitive to both mechanisms. |
1(0,0,0,1) | Details |