Increase of human platelet serotonin uptake by atypical histamine receptors.
Increase of human platelet serotonin uptake by atypical histamine receptors.
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非典型组胺受体增加人血小板血清素的摄取。
DOI：
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发表时间：
1994
影响因子：
--
通讯作者：
Christian Gespach
中科院分区：
文献类型：
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作者：
Jean;D. Bondoux;M.;S. Emami;V. Mutel;M. Haimart;Christian Gespach
组胺和鸟苷3′，5′-环单磷酸（cGMP）诱导剂硝普钠均能提高离体人血小板中5-羟色胺（5- ht）的摄取和cGMP水平。在10 nM至0.25微米的浓度范围内观察到组胺能刺激[平均有效浓度(EC50) = 0.1微米组胺]。H2受体拮抗剂硫替丁、甲胺和西咪替丁对人血小板中调节5-羟色胺摄取和cGMP生成的组胺受体的抑制作用是其他组织中组胺能受体H1、HIC、H2和H3的10-10(5)倍。体外组胺诱导的5-羟色胺摄取可以通过在一氧化氮合酶抑制剂ng -单甲基-l -精氨酸或cgmp降低剂LY-83583中预孵育分离的人血小板来阻止。组胺在刺激人血小板cAMP生成方面无效，并且不与已知下调5-羟色胺摄取的效应位点相互作用，包括丙咪嗪、γ -氨基丁酸A、外周型苯二氮卓结合位点和诱导人血小板形状改变和聚集的V1a抗利尿激素受体。这些非典型人血小板组胺能受体与先前分类的组胺受体不同，它们对组胺h2受体拮抗剂具有明显的高亲和力，并且与可溶性的、依赖一氧化氮的鸟苷酸环化酶有明显的联系。这些发现提示人类血小板表达一种新的组胺受体亚型H2h。
Histamine and the guanosine 3',5'-cyclic monophosphate (cGMP)-inducing agent sodium nitroprusside both increased serotonin (5-HT) uptake and cGMP levels in isolated human platelets in vitro. Histaminergic stimulation was observed at concentrations ranging from 10 nM to 0.25 microM [mean effective concentration (EC50) = 0.1 microM histamine]. The inhibition produced by the H2-receptor antagonists tiotidine, metiamide, and cimetidine was 10-10(5) times more potent on histamine receptors regulating 5-HT uptake and cGMP generation in human platelets than on the histaminergic receptors H1, HIC, H2, and H3 in other tissues. The in vitro histamine-induced 5-HT uptake was prevented by preincubation of isolated human platelets in the presence of the nitric oxide synthase inhibitor NG-monomethyl-L-arginine or the cGMP-lowering agent LY-83583. Histamine was ineffective in stimulating cAMP generation in human platelets and did not interact with effector sites known to downregulate 5-HT uptake, including imipramine, gamma-aminobutyric acid A, peripheral type benzodiazepine-binding sites, and V1a vasopressin receptors inducing human platelet shape change and aggregation. These atypical human platelet histaminergic receptors differ from the previously classified histamine receptors by their apparent high affinity to histamine H2-receptor antagonists and their apparent link with the soluble, nitric oxide-dependent guanylate cyclase. These findings suggest that human platelets express a new subtype H2h of histamine receptors.
影响因子：
56.9
作者：
LIGHT, DB;SCHWIEBERT, EM;STANTON, BA
通讯作者：
STANTON, BA