Protein Information

Name NK 1
Synonyms B3GAT1; CD57; CD57 antigen; GLCATP; Galactosylgalactosylxylosylprotein 3 beta glucuronosyltransferase 1; GlcAT I; GlcAT P; GlcUAT P…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
12372532 Ryckmans T, Berton O, Grimee R, Kogej T, Lamberty Y, Pasau P, Talaga P, Genicot C: Dual NK (1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3195-8.

The synthesis, structure-affinity relationship and activity of benzyloxyphenethyl piperazine derivatives combining NK (1) antagonism and serotonin reuptake inhibition is described.
82(1,1,1,2) Details
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} -acetic acid [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} -acetic acid [(11) C] methyl ester ([(11) C] BME, [(11) C]) were synthesized for evaluation as new potential PET imaging agents for brain NK (1) receptors.
81(1,1,1,1) Details
12372524 Blythin DJ, Chen X, Piwinski JJ, Shih NY, Shue HJ, Anthes JC, McPhail AT: Synthesis and NK (1)/NK (2) binding activities of a series of diacyl-substituted 2-arylpiperazines. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3161-5.

X-ray crystallographic analysis of the crystalline di-BOC derivative of the NK (2) active piperazine (15) showed that the 2R configuration was associated with NK (2) activity.
4(0,0,0,4) 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.
4(0,0,0,4) Details
11714604 Shaw D, Chicchi GG, Elliott JM, Kurtz M, Morrison D, Ridgill MP, Szeto N, Watt AP, Williams AR, Swain CJ: 2-Aryl indole NK (1) antagonists: optimisation of the amide substituent. Bioorg Med Chem Lett. 2001 Dec 3;11(23):3031-4.

The 1-(2-methoxyphenyl) piperazine amide was identified as a major area of metabolism in the lead compound 1.
2(0,0,0,2) Details