[3H]Yohimbine binding to human platelet membranes: evidence for high and low affinity binding sites with negative cooperativity.
[3H]Yohimbine binding to human platelet membranes: evidence for high and low affinity binding sites with negative cooperativity.
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[3H]育亨宾与人血小板膜的结合:高和低亲和力结合位点具有负协同性的证据。
DOI:
10.1016/0014-2999(85)90180-3
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发表时间:
1985
影响因子:
5
通讯作者:
P. Somani
中科院分区:
文献类型:
--
作者:
S. Periyasamy;P. Somani
Evidence is presented that [3H]yohimbine binding to human platelet does not follow the simple mass action kinetics. Although [3H]yohimbine binding was saturable and stereospecific, Scatchard analysis of the equilibrium binding data produced a curvilinear plot. Competitive displacement of [3H]yohimbine from the binding sites by unlabeled yohimbine and other α2-antagonists produced shallow inhibition curves. Further, the apparent Hill coefficients of equilibrium binding and competitive displacement data were found to be less than unity. Factors such as binding to nonreceptor sites or to α1-adrenoceptors, dopamine receptors, or 5-HT receptors that may explain the curvilinear curve were excluded. The rank order of potency for inhibiting [3H]yohimbine was rauwolscine > yohimbine > phentolamine > clonidine ⋙ prazosin, suggesting that the binding sites had the characteristics of α2-adrenoreceptors. The affinity of the α2-antagonist for the receptor was enhanced by Na+but not by guanine nucleotide, suggesting that the binding of the antagonist is modulated only by Na+. Graphic analysis of the specific binding data resulted in two components: one with high affinity and low capacity sites, and second with low affinity and high capacity sites. The experiments on dissociation kinetics, however, suggest that the observed deviation of [3H]yohimbine binding from the simple mass action kinetics is most likely due to negative cooperative interactions among α2-adrenoceptor sites.
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DOI:
10.1073/pnas.77.8.4569
发表时间:
1980
影响因子:
11.1
作者:
Hoffman,BB;Michel,T;Kilpatrick,DM;Lefkowitz,RJ;Tolbert,ME;Gilman,H;Fain,JN
通讯作者:
Fain,JN
影响因子:
5.8
作者:
Panosian,JO;Marinetti,GV
通讯作者:
Marinetti,GV
DOI:
--
发表时间:
1981
期刊:
Journal of cyclic nucleotide research
影响因子:
--
作者:
Wolfe,BB;Harden,TK
通讯作者:
Harden,TK
DOI:
--
发表时间:
1984
期刊:
The Journal of pharmacology and experimental therapeutics
影响因子:
--
作者:
Martin,MW;Smith,MM;Harden,TK
通讯作者:
Harden,TK
影响因子:
3.6
作者:
Limbird,LE;Speck,JL;Smith,SK
通讯作者:
Smith,SK