The novel potent multidrug resistance inhibitors n,n-bis(cyclohexanol)amine aryl esters are devoid of vascular effects

Pharmacology

Volumn 88, Issue 3-4, 2011, Pages 137-141

  Saponara, Simona ^a,b   Gorelli, Beatrice ^a,b   Tzankova, Virginia ^d   Martelli, Cecilia ^c   Teodori, Elisabetta ^c   Sgaragli, Giampietro ^a,b   Fusi, Fabio ^a,b  

^a UNIVERSITY OF SIENA   (Italy)

^b ISTITUTO TOSCANO TUMORI   (Italy)

^c UNIVERSITY OF FLORENCE   (Italy)

^d MEDICAL UNIVERSITY OF SOFIA   (Bulgaria)

Author keywords

N,N bis(cyclohexanol)amine aryl esters; Rat aorta; Rat tail artery myocytes; Whole cell patch clamp

Indexed keywords

3,4,5 TRIMETHOXYBENZOIC ACID 4 (METHYL [4 [3 (3,4,5 TRIMETHOXYPHENYL)ACRYLOYLOXY]CYCLOHEXYL]AMINO)CYCLOHEXYL ESTER; BARIUM ION; CALCIUM CHANNEL; CYCLOHEXANOL DERIVATIVE; PHENYLEPHRINE; UNCLASSIFIED DRUG; VASODILATOR AGENT; VERAPAMIL;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CARDIOVASCULAR EFFECT; CARDIOVASCULAR FUNCTION; DRUG EFFECT; DRUG MECHANISM; DRUG POTENCY; ELECTROPHYSIOLOGY; ENDOTHELIUM; HEART MUSCLE CELL; IN VITRO STUDY; MALE; MULTIDRUG RESISTANCE; NONHUMAN; PRIORITY JOURNAL; RAT; TAIL ARTERY; VASCULAR RING;

ANIMALS; AORTA; ARTERIES; CALCIUM CHANNEL BLOCKERS; DRUG RESISTANCE, MULTIPLE; ESTERS; MALE; MYOCYTES, SMOOTH MUSCLE; P-GLYCOPROTEIN; PATCH-CLAMP TECHNIQUES; RATS; RATS, WISTAR; TAIL; VASODILATION; VERAPAMIL;

EID: 80052674050     PISSN: 00317012     EISSN: 14230313     Source Type: Journal    
DOI: 10.1159/000330452     Document Type: Article

References (14)

1. Gottesman MM, Fojo T, Bates SE: Multidrug resistance in cancer: role of ATP-dependent transporters. Nature Rev Cancer 2002; 2: 48-58. (Pubitemid 37328807)
2. Johnstone RW, Ruefli AA, Smyth MJ: Multiple physiological functions for multidrug transporter P-glycoprotein? Trends Biochem Sci 2000; 25: 1-6. (Pubitemid 30060419)
3. Bellamy WT: P-glycoproteins and multidrug resistance. Annu Rev Pharmacol Toxicol 1996; 36: 161-183. (Pubitemid 26169898)
4. Martelli C, Alderighi D, Coronnello M, Dei S, Frosini M, le Bozec B, Manetti D, Neri A, Romanelli MN, Salerno M, Scapecchi S, Mini E, Sgaragli G, Teodori E: N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors. J Med Chem 2009; 52: 807-817.
5. Zolnerciks JK, Wooding C, Linton KJ: Evidence for a Sav1866-like architecture for the human multidrug transporter P-glycoprotein. FASEB J 2007; 21: 3937-3948. (Pubitemid 350232351)
6. Globish C, Pajeva IK, Wiese M: Identification of putative binding sits of P-glycoprotein based on its homology models. ChemMedChem 2008; 3: 280-295.
7. Murray DS, Schumacher MA, Brennan RG: Crystal structure of QacR-diamidine complexes reveal additional multidrug-binding modes and a novel mechanism of drug charge neutralization. J Biol Chem 2004; 279: 14365-14371. (Pubitemid 38468978)
8. Schumacher MA, Miller MC, Brennan RG: Structural mechanism of the simultaneous binding of two drugs to a multidrug binding protein. EMBO J 2004; 23: 2923-2930. (Pubitemid 39093587)
9. Aller SG, Yu J, Ward A, Weng Y, Chittaboina S, Zhuo R, Harrell PM, Trinh YT, Zhang Q, Urbatsch IL, Chang G: Structure of P-glycoprotein reveals a molecular basis for polyspecific drug binding. Science 2009; 323: 1718-1722.
10. Fusi F, Marazova K, Pessina F, Gorelli B, Valoti M, Frosini M, Sgaragli GP: On the mechanisms of the antispasmodic action of some hindered phenols in rat aorta rings. Eur J Pharmacol 2000; 394: 109-115. (Pubitemid 30193296)
11. Fusi F, Saponara S, Gagov H, Sgaragli GP: 2,5-Di-t-butyl-1,4- benzohydroquinone (BHQ) inhibits vascular L-type Ca 2+ channel via superoxide anion generation. Br J Pharmacol 2001; 133: 988-996.
12. Hamill OP, Marty A, Neher E, Sakmann B, Sigworth FJ: Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches. Pflugers Arch 1981; 391: 85-100. (Pubitemid 11012976)
13. McFadzean I, Gibson A: The developing relationship between receptor-operated and store-operated calcium channels in smooth muscle. Br J Pharmacol 2002; 135: 1-13. (Pubitemid 34103011)
14. Gurney AM: Mechanisms of drug-induced vasodilation. J Pharm Pharmacol 1994; 46: 242-251. (Pubitemid 24111127)