首页> 外文期刊>The Journal of Physiology >Antagonists of the cGMP-gated conductance of vertebrate rods block the photocurrent in scallop ciliary photoreceptors.
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Antagonists of the cGMP-gated conductance of vertebrate rods block the photocurrent in scallop ciliary photoreceptors.

机译:脊椎动物杆的cGMP门控电导的拮抗剂阻断了扇贝睫状感光器中的光电流。

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摘要

1. Hyperpolarizing scallop photoreceptors, like vertebrate rods, use cGMP as an internal messenger and their light-sensing structure is also of ciliary origin. To ascertain possible functional similarities between the light-sensitive conductances in the two classes of visual cells, we examined in scallop photoreceptors the effects of several antagonists of the photocurrent of rods. 2. Extracellular application of L-cis-diltiazem rapidly and reversibly suppressed the photocurrent. The effect was stereospecific and dose dependent, with a K1/2 of approximately 400 microM. Intracellular dialysis at lower doses (100-200 microM) also induced a substantial inhibition. 3. L-cis-Diltiazem reduced the light-activated conductance without shifting the intensity-response curve. Furthermore, the drug also blocked the current directly evoked by application of cGMP. These observations indicate that the inhibitory effects result from blockage of the conductance, rather than from impairment of the activating cascade. 4.The fractional blockage increased e-fold per approximately 55 mV depolarization, regardless of the side of drug application, as if the charged form of L-cis-diltiazem can only access the blocking site from the intracellular compartment. 5. The amiloride derivative 3',4'-dichlorobenzamil potently suppressed the photocurrent (K1/2 approximately 5 microM), without affecting its kinetics or operating range. Amiloride itself was also effective at higher concentrations. 6. The pharmacological resemblance of these light-dependent channels to those of rods and cones indicates that significant aspects of the transduction cascade are conserved across disparate sensory cells of ciliary origin.
机译:1.超极化的扇贝感光体,像脊椎动物的棒一样,使用cGMP作为内部信使,它们的光敏结构也是睫状起源的。为了确定两类视觉细胞中光敏电导之间可能的功能相似性,我们在扇贝感光器中检查了几种棒状光电流拮抗剂的作用。 2.在细胞外应用L-顺-地尔硫卓快速可逆地抑制光电流。效果是立体特异性的,并且是剂量依赖性的,K1 / 2约为400 microM。较低剂量(100-200 microM)的细胞内透析也诱导了实质性的抑制作用。 3. L-顺式-地尔硫卓降低了光激活电导,而没有改变强度响应曲线。此外,该药物还阻止了通过应用cGMP直接引起的电流。这些观察结果表明抑制作用是由电导的阻滞而不是由活化级联的损伤引起的。 4,无论药物应用的哪一面,每约55 mV的去极化,部分阻滞剂的e倍增加,似乎L-顺式-地尔硫ze的带电荷形式只能从细胞内区室进入阻滞位点。 5.阿米洛利衍生物3',4'-dichlorobenzamil有效抑制光电流(K1 / 2约5 microM),而不会影响其动力学或操作范围。阿米洛利本身在较高浓度下也有效。 6.这些光依赖性通道与棒状和锥状通道的药理学相似性表明,跨睫状起源的不同感觉细胞,转导级联反应的重要方面得以保留。

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