Characterization of histamine type 1 receptors on natural suppressor lymphoid cells.
Characterization of histamine type 1 receptors on natural suppressor lymphoid cells.
复制标题
天然抑制性淋巴细胞上组胺 1 型受体的表征。
DOI：
10.1016/0006-2952(87)90451-5
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发表时间：
1987
影响因子：
5.8
通讯作者：
Melmon,KL
中科院分区：
文献类型：
--
作者：
Khan,MM;Wilson,AL;Melmon,KL
利用放射性配体h1拮抗剂[3H]吡咯胺，我们对克隆小鼠自然抑制细胞（NS）上的组胺1型受体进行了表征。[3H]吡啶胺的单一特异性结合位点存在于这些细胞上。这种结合是饱和的，并且可以被各种特异性的h1受体拮抗剂逆转。h1受体拮抗剂取代[3H]吡咯胺与h1受体结合的效价顺序为异丙嗪=邻苯丁胺>吡咯胺>苯海拉明>氯苯那敏。组胺2型激动剂丙咪嘧啶和地马匹利，拮抗剂西咪替丁和雷尼替丁，以及选定的非组胺激动剂，并没有取代天然抑制细胞上的[3H]吡啶胺的结合位点。结果表明，[3H]吡啶胺的理论结合度为1.1±0.3 × 10−7M，而实际结合度为6.0±0.8 × 10−8M；最大结合深度为4.13 nM，结合位点数为2.14±0.29 × 106个/细胞（N = 3）。
Using the radioligand H1antagonist [3H]pyrilamine, we have characterized the histamine type 1 receptor on cloned murine natural suppressor cells (NS). A single, specific binding site for [3H]pyrilamine exists on these cells. The binding was saturable and reversible by various specific H1receptor antagonists. The rank order of potency for displacement of [3H]pyrilamine binding from the H1receptor by H1receptor antagonists was promethazine = pyrobutamine > pyrilamine > diphenhydramine > chlorpheniramine. The histamine type-2 agonists, impromidine and dimaprit, and antagonists, cimetidine and ranitidine, as well as selected non-histamine agonists, did not displace [3H]pyrilamine from its binding sites on the natural suppressor cells. The data indicate that the theoreticalKDwas 1.1 ± 0.3 × 10−7M while the measuredKDof binding for [3H]pyrilamine was 6.0 ± 0.8 × 10−8M; the maximum binding was 4.13 nM and the number of binding sites/cell was 2.14 ± 0.29 × 106(N = 3).