硫替丁(Tiotidine) - 药物靶点：H2 receptor_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

H2 receptor

作用机制

H2 receptor拮抗剂(组胺H2受体拮抗剂)

治疗领域-

在研适应症-

非在研适应症-

原研机构

Imperial Chemical Industries Ltd.

在研机构

Imperial Chemical Industries Ltd.

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C10H16N8S2

InChIKeyYDDXVAXDYKBWDX-UHFFFAOYSA-N

CAS号69014-14-8

关联

100 项与硫替丁相关的临床结果

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100 项与硫替丁相关的转化医学

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100 项与硫替丁相关的专利（医药）

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1

项与硫替丁相关的文献（医药）

2007-11-15·Journal of Experimental Biology2区 · 生物学

Histamine operates Cl–-gated channels in crayfish neurosecretory cells

2区 · 生物学

Article

作者: García, Ubaldo ; Cebada, Jorge

SUMMARYWe describe a histamine-activated Cl– conductance in the X-organ neurons from crayfish Cherax quadricarinatus, which has comparable properties to the homomultimeric histamine-gated ion channels described in Drosophila. Topical application of histamine inhibited spontaneous neuronal firing in the X-organ sinus gland tract, concomitant with an increase in the membrane conductance. In X-organ neurons in culture and under voltage-clamp conditions, histamine evoked outward currents at –40 mV that reversed at the Cl– equilibrium potential. Histamine sensitivity in these neurons had a half-maximal response(EC50)=3.3±1 μmol l–1, with a Hill number of 2.6±0.4. The histamine-evoked current was blocked by tiotidine, cimetidine, ranitidine and 256±11 and 483±11 μmol l–1, respectively) and d-tubocurarine(IC50=21±2 μmol l–1), but was insensitive to picrotoxin, bicuculline and strychnine. Neither GABA nor glutamate was capable of desensitizing the histamine response, indicating that histamine activates a particular Cl– conductance. The presence of immunoreactive neurons to histamine in the medulla terminalis with axonal projections to the neuropile suggests a possible histaminergic modulation of the X-organ sinus gland system.

100 项与硫替丁相关的药物交易

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