Stimulation by alkylxanthines of chloride efflux in CFPAC-1 cells does not involve A1 adenosine receptors.
Stimulation by alkylxanthines of chloride efflux in CFPAC-1 cells does not involve A1 adenosine receptors.
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CFPAC-1 细胞中烷基黄嘌呤对氯离子流出的刺激不涉及 A1 腺苷受体。
DOI：
10.1021/bi00028a018
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发表时间：
1995
期刊：
影响因子：
2.9
通讯作者：
Pollard,HB
中科院分区：
文献类型：
--
作者：
Jacobson,KA;Guay-Broder,C;vanGalen,PJ;Gallo-Rodriguez,C;Melman,N;Jacobson,MA;Eidelman,O;Pollard,HB
Revised Manuscript Received April 28, 1995® abstract: A series of 8-substituted derivatives of 1, 3, 7-alkylxanthines was synthesized as potential activators of chloride efflux from a human epithelial cell line (CFPAC) expressing the cystic fibrosis transmembrane regulator (CFTR) AF508 mutation. Their interactions with rat brain Ai and A2a receptors were also studied in radioligand binding experiments. Substitution was varied at thexanthine 1-, 3-, 7-and 8-positions. l, 3-Dipropyl-8-cyclopentylxanthine (CPX) stimulated Cl-efflux in the 10-8 M range, with a maximal effect reaching 200% of control and diminishing at higher concentrations. The potent adenosine antagonist 8-[4-[[[[(2-aminoethyl) amino] carbonyl] methyl] oxy] phenyl]-l, 3-dipropylxanthine, nonselective at human Ai and A2a receptors, was inactive in Cl" efflux. l, 3-Diallyl-8-cyclohexylxanthine (DAX) was highly efficacious in stimulating chloride efflux with levels reaching> 300% of control, although micromolar concentrations were required. l, 3, 7-Trimethyl-8-(3-chlorostyryl) xanthine, an A2a-selective adenosine antagonist, was only weakly active. Caffeine, which acts as an nonselective adenosine antagonist in the range of 10-5 M, was active in Cl-efflux in the low nanomolar range but with low efficacy. Thus, among the xanthine derivatives of diverse structure, there was no correlation between potency in Cl-efflux and adenosine antagonism. Poly (A)-F RNA isolated from CFPAC-1 cellsshowed no hybridization to a human Ai receptor cDNA probe, excluding this receptor as a mediator of CPX-elicited Cl efflux. Thus, this action of xanthines in a defective CFTR, represents a novel site ofCystic fibrosis is the most common genetic disease among the Caucasian population (Boat et al., 1989) and is character-ized by a defect in the 3', 5'-cyclic AMP-activated chloride efflux from affected epithelial cells (Welsh, 1990; Quinton, 1990) and by abnormal mucin secretion in the lungs, intestines, and other affected organs (Boat et al, 1989). The molecular basis of this diseasehas been traced to specific mutations in the cystic fibrosis transmembrane regulator
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DOI：
10.1073/pnas.89.16.7432
发表时间：
1992-08-15
影响因子：
11.1
作者：
ZHOU, QY;LI, CY;CIVELLI, O
通讯作者：
CIVELLI, O
通过嘌呤受体起作用的新疗法。
影响因子：
5.8
作者：
Jacobson,KA;Trivedi,BK;Churchill,PC;Williams,M
通讯作者：
Williams,M
三氟甲基和其他取代基对腺苷受体黄嘌呤活性的影响。
影响因子：
7.3
作者：
Jacobson,KA;Shi,D;Gallo-Rodriguez,C;ManningJr,M;Müller,C;Daly,JW;Neumeyer,JL;Kiriasis,L;Pfleiderer,W
通讯作者：
Pfleiderer,W
影响因子：
56.9
作者：
J. Riordan;J. Rommens;N. Alon;R. Rozmahel;Z. Grzelczak;J. Zieleński;N. Plavsic;Jia-Ling Chou
通讯作者：
J. Riordan;J. Rommens;N. Alon;R. Rozmahel;Z. Grzelczak;J. Zieleński;N. Plavsic;Jia-Ling Chou
8-苯基和 8-环烷基取代基对 1-、3-和 7-位取代的单、二和三取代烷基黄嘌呤活性的影响。
影响因子：
7.3
作者：
M. Shamim;Dieter Ukena;W. Padgett;John W. Daly
通讯作者：
John W. Daly