| Name | neurokinin 1 |
|---|---|
| Synonyms | Hs.2563; PPT; NK2; NKA; NKNA; Neurokinin 1; Neurokinin 2; Neurokinin A… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 15005884 | Leopoldo M, Berardi F, Colabufo NA, Contino M, Lacivita E, Perrone R, Tortorella V: Studies on 1-arylpiperazine derivatives with affinity for rat 5-HT7 and 5-HT1A receptors. J Pharm Pharmacol. 2004 Feb;56(2):247-55. Intrinsic activity of the most potent compounds was assessed. 4-[2-(3-Methoxyphenyl) ethyl]-1-(2-methoxyphenyl) piperazine (16) and 1-(1,2-benzisoxazol-3-yl)-4-[2-(3-methoxyphenyl) ethyl] piperazine (20) (K (i) = 24.5 and 8.2 nM, respectively) behaved as partial agonist and full agonist, respectively, when tested for 5-HT (7) receptor-mediated relaxation of substance P-induced guinea-pig ileum contraction. |
31(0,1,1,1) | Details |
| 12570387 | Perrone R, Berardi F, Colabufo NA, Lacivita E, Leopoldo M, Tortorella V: Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl) alkyl]-1-aryl ketones as 5-HT (7) receptor ligands. J Med Chem. 2003 Feb 13;46(4):646-9. The presence of a or methoxy substituent on aryl ketone moiety, alkyl chain length, and the nature of N-1-piperazine substituent were explored. 6-[4-(3-Benzisoxazolyl)-1-piperazinyl]-1-(2-hydroxyphenyl)-1- (40) and its methoxy analogue 43 exhibited high 5-HT (7) receptor affinities (Ki = 2.93 nM and 0.90 nM, respectively) and agonist properties when tested for 5-HT (7) receptor-mediated relaxation of substance P-induced guinea-pig ileum contraction. |
31(0,1,1,1) | Details |
| 12431064 | MacKenzie AR, Marchington AP, Middleton DS, Newman SD, Jones BC: Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)- 5-[2-[(3-substituted)-1-azetidinyl] ethyl]-2-piperidones. 1. J Med Chem. 2002 Nov 21;45(24):5365-77. The design, synthesis, and pharmacological evaluation of a novel class of neurokinin-2 (NK2) antagonists 1-alkyl-5-(3,4-dichlorophenyl)-5-[2-[(3-substituted)-1-azetidinyl] ethyl]-2 -piperidones (5-44) are described. |
3(0,0,0,3) | 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. |
2(0,0,0,2) | Details |
| 11311404 | Yonehara N: Influence of serotonin receptor antagonists on substance P and release evoked by tooth pulp stimulation with electro-acupuncture in the trigeminal nucleus cudalis of the rabbit. Neurosci Res. 2001 May;40(1):45-51. |
2(0,0,0,2) | Details |
| 11745625 | Hu HZ, Gao N, Lin Z, Gao C, Liu S, Ren J, Xia Y, Wood JD: P2X (7) receptors in the enteric nervous system of guinea-pig small intestine. J Comp Neurol. 2001 Nov 19;440(3):299-310. P2X (7) immunoreactivity was colocalized with synapsin and synaptophysin and surrounded ganglion cells that contained either calbindin, calretinin, neuropeptide Y, substance P, or synthase. The P2X (7) antagonists 1-[N,O-bis (1,5-isoquinolinesulfonyl)-N-methyl-l-tyrosyl]-4-piperazine (KN-62) and oxidized ATP also suppressed the BzBzATP-activated current. |
1(0,0,0,1) | Details |
| 15588097 | Leopoldo M, Berardi F, Colabufo NA, Contino M, Lacivita E, Niso M, Perrone R, Tortorella V: Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents. J Med Chem. 2004 Dec 16;47(26):6616-24. In relation to 5-HT7 receptor affinity, receptor binding studies indicated that (i) the optimal alkyl chain length was five methylenes, (ii) an unsubstituted 1,2,3,4-tetrahydronaphthalenyl nucleus was preferred, and (iii) the substitution pattern of the aryl ring linked to the piperazine ring played a crucial role. Among them, 4-(2-methoxyphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazinehexa namide (28), 4-(2-acetylphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazinehexan amide (34), 4-(2-methylthiophenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazineh exanamide (44), 4-(2-hydroxyphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazinehexa namide (46), and 4-(2-methylphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazinehexan amide (49) were assayed for the 5-HT7 receptor-mediated relaxation of substance P-induced guinea pig ileum contraction. |
1(0,0,0,1) | Details |
| 15895105 | Weston AH, Feletou M, Vanhoutte PM, Falck JR, Campbell WB, Edwards G: Bradykinin-induced, endothelium-dependent responses in porcine coronary arteries: involvement of potassium channel activation and epoxyeicosatrienoic acids. Br J Pharmacol. 2005 Jul;145(6):775-84. Hyperpolarization of endothelial cells by bradykinin (27.0 +/- 0.9 mV, n = 4) was partially inhibited (74%) by blockade of IK (Ca) and SK (Ca) channels using 10 microM TRAM-39 (2-(2-chlorophenyl)-2,2-diphenylacetonitrile) plus 100 nM apamin (leaving an iberiotoxin-sensitive component), whereas the response to substance P was abolished. After gap junction blockade with HEPES, (N-(2-hydroxyethyl) piperazine-N'-(2-ethanesulphonic acid)) hyperpolarization of the endothelium by 100 nM bradykinin was abolished by TRAM-39 plus apamin, whereas myocyte hyperpolarization still occurred (12.9 +/- 1.0 mV, n=4). |
1(0,0,0,1) | Details |
| 11121732 | Beaumont K, Harper A, Smith DA, Bennett J: The role of P-glycoprotein in determining the oral absorption and clearance of the NK2 antagonist, UK-224,671. Eur J Pharm Sci. 2000 Nov;12(1):41-50. |
1(0,0,0,1) | Details |