ALPHA-2-ADRENOCEPTORS IN HOMOGENATES OF RAT NASAL-MUCOSA

被引:4
|
作者
VANMEGEN, YJB
DEMIRANDA, JFR
KLAASSEN, ABM
WENTGES, BTR
VANGINNEKEN, CAM
机构
[1] CATHOLIC UNIV NIJMEGEN, DEPT PHARMACOL, NIJMEGEN, NETHERLANDS
[2] CATHOLIC UNIV NIJMEGEN, DEPT OTORHINOLARYNGOL, NIJMEGEN, NETHERLANDS
关键词
(Non-linear non-specific binding); (Subtypes); Nasal mucosa; [!sup]3[!/sup]H]Rauwolscine binding; α[!sub]2[!/sub]-Adrenoceptors;
D O I
10.1016/0014-2999(90)90056-C
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The specific binding of [3H]rauwolscine to rat nasal mucosa membranes was saturable, stereoselective and of high affinity. The Scatchard plot pointed to a homogeneous population of binding sites (Kd = 3.6 ± 0.6 nM; Bmax = 5.1 ± 0.7 pmol/g). The non-specific binding appeared to be non-linear, probably due to filter binding. Inhibition of [3H]rauwolscine binding with the subtype-selective antagonist, prazosin, suggested the presence of α2-adrenoceptor subclasses in rat nasal mucosa. The (-)-epinephrine inhibition curves demonstrated high- and low-affinity agonist binding sites. A monophasic (-)-epinephrine inhibition curve was obtained in the presence of guanine nucleotides. © 1990.
引用
收藏
页码:561 / 567
页数:7
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