| Name | P glycoprotein |
|---|---|
| Synonyms | ABC20; MDR1; ABCB 1; ABCB1; ATP binding cassette sub family B member 1; CD243; CD243 antigen; CLCS… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 12649383 | Cummins CL, Salphati L, Reid MJ, Benet LZ: In vivo modulation of intestinal CYP3A metabolism by P-glycoprotein: studies using the rat single-pass intestinal perfusion model. J Pharmacol Exp Ther. 2003 Apr;305(1):306-14. N-Methyl piperazine--homoPhe-vinylsulfone phenyl (K77), a peptidomimetic protease inhibitor (CYP3A/P-gp substrate), and midazolam (CYP3A substrate) were each perfused through a segment of rat ileum alone and with the P-gp inhibitor N-(4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)-ethyl]-phenyl)- 9,10-dihydro-5-methoxy-9-oxo-4-acridine carboxamine (GG918). |
84(1,1,1,4) | Details |
| 11861813 | Cummins CL, Jacobsen W, Benet LZ: Unmasking the dynamic interplay between intestinal P-glycoprotein and CYP3A4. J Pharmacol Exp Ther. 2002 Mar;300(3):1036-45. The transport, metabolism, and intracellular levels of N-methyl piperazine--homoPhe-vinylsulfone phenyl (K77, a protease inhibitor; P-gp and CYP3A4 substrate) and felodipine (CYP3A4 substrate only) were measured across CYP3A4-transfected Caco-2 cells in the presence of an inhibitor of CYP3A4 and P-gp, cyclosporine (CsA), or an inhibitor of P-gp and not CYP3A4, GG918 (N-[4-[2-(1,2,3,4-tetrahydro-6,7- dimethoxy-2-isoquinolinyl)-ethyl]-phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-a cridine carboxamine). |
6(0,0,0,6) | Details |
| 11068023 | Passchier J, van Waarde A, Doze P, Elsinga PH, Vaalburg W: Influence of P-glycoprotein on brain uptake of [18F] MPPF in rats. Eur J Pharmacol. 2000 Nov 3;407(3):273-80. Anesthetized male Wistar rats were injected i.v. with the 5-HT1A receptor antagonist [18F] MPPF (2 MBq, S.A.> 110 TBq/mmol) after treatment with saline (controls) or with the 5-HT1A receptor antagonist 1-(2'-methoxyphenyl)-4-[4-(2-phthalimido) butyl] piperazine (NAN-190) (2.5 mg/kg i.v.). |
5(0,0,0,5) | 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. |
5(0,0,0,5) | Details |
| 12423172 | Andrus MB, Mettath SN, Song C: A modified synthesis of iodoazidoaryl prazosin. . J Org Chem. 2002 Nov 15;67(23):8284-6. The antihypertension agent iodoazidoaryl prazosin (IAAP) has been made using a convergent route involving addition of an acylated piperazine 7 to 2-chloroquinazoline 5. IAAP has been shown to function as a multidrug resistance (MDR) reversal agent and bind to P-glycoprotein, a transmembrane transport protein. |
1(0,0,0,1) | Details |
| 15727877 | Shchekotikhin AE, Shtil AA, Luzikov YN, Bobrysheva TV, Buyanov VN, Preobrazhenskaya MN: 3-Aminomethyl derivatives of 4,11-dihydroxynaphtho [2,3-f] -5,10-dione for circumvention of anticancer drug resistance. Bioorg Med Chem. 2005 Mar 15;13(6):2285-91. The potency of novel derivatives was tested on a National Cancer Institute panel of 60 human tumor cell lines as well as in cells with genetically defined determinants of cytotoxic drug resistance, P-glycoprotein (Pgp) expression, and p53 inactivation. We conclude that Mannich modification of 4,11-dihydroxynaphtho [2,3-f] -5,10-dione, especially when cyclic diamine (e.g., piperazine, quinuclidine) is used, confers an important feature to the resulting compounds, namely, the potency for tumor cells otherwise resistant to a variety of anticancer drugs. |
1(0,0,0,1) | Details |
| 11311063 | Gamage SA, Spicer JA, Finlay GJ, Stewart AJ, Charlton P, Baguley BC, Denny WA: Dicationic bis (9-methylphenazine-1-carboxamides): relationships between biological activity and linker chain structure for a series of potent topoisomerase targeted anticancer drugs. J Med Chem. 2001 Apr 26;44(9):1407-15. Representative compounds were susceptible to transport mediated resistance, being much less effective in cells that overexpressed P-glycoprotein. Constraining the rigidity of the linker chain by incorporating a piperazine ring did not decrease potency significantly. |
1(0,0,0,1) | Details |
| 18781943 | Chen C: Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines and levocetirizine. Curr Med Chem. 2008;15(21):2173-91. is a piperazine derivative related to the first generation H (1) antagonist hydroxyzine, and is the major metabolite in the blood circulation after hydroxyzine administration in humans. For example, has much lower CNS penetration than hydroxyzine, which may be explained by the zwitterionic structure of and its P-glycoprotein activity. |
1(0,0,0,1) | Details |
| 16152590 | Weiderhold KN, Randall-Hlubek DA, Polin LA, Hamel E, Mooberry SL: CB694, a novel antimitotic with antitumor activities. Int J Cancer. 2006 Feb 15;118(4):1032-40. During the course of a mechanism-based screening program aimed at identifying new antimitotic agents, a novel microtubule depolymerizing piperazine derivative, 1-(5-chloro-2-methoxybenzoyl)-4-(3-chlorophenyl) piperazine, was identified. A multidrug-resistant cell line was sensitive to inhibition by CB694, suggesting that this compound is a poor substrate for transport by P-glycoprotein. |
1(0,0,0,1) | Details |