更新于：2024-11-01

Scorpion venoms

更新于：2024-11-01

基本信息

别名-

简介-

关联

项与 Scorpion venoms 相关的药物

Centruroides (scorpion) immune F(ab)2(Rare Disease Therapeutics, Inc.)

靶点

Scorpion venoms

作用机制

蝎毒液类抑制剂

在研机构

Rare Disease Therapeutics, Inc.

原研机构

Rare Disease Therapeutics, Inc.

在研适应症

蝎子叮咬

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区

美国

首次获批日期2011-08-03

项与 Scorpion venoms 相关的临床试验

NCT01599923 / Completed临床3期

Open Label, Confirmatory, Controlled Clinical Study of Alacramyn® in Pediatric Patients With Scorpion Sting Envenomation

There is no FDA approved therapy for the treatment of scorpion envenomation in the United States. Centruroides scorpion envenomation produces a pattern of neurotoxicity with a spectrum of severity ranging from trivial to life threatening. Patients stung by Centruroides scorpions develop a clinical syndrome which may require sedation with benzodiazepines and observation for 6 to 28 hours of intensive care monitoring. A safe therapy is necessary to halt the progression of symptoms early in the clinical course while avoiding the clinical deterioration that can occur en route to a tertiary facility. Alacramyn® is anticipated to be safer and more effective than the present standard of care in the United States, midazolam, and faster-acting thus eliminating the need to transport most rural patients and reducing hospitalization time.

开始日期2005-05-01

申办/合作机构

Instituto Bioclon SA de CV

[+2]

NCT01599936 / Completed临床3期

Open Label, Confirmatory, Controlled Clinical Study of Alacramyn® in Pediatric Patients With Scorpion Sting Envenomation

There is no FDA approved therapy for the treatment of scorpion envenomation. Centruroides scorpion envenomation produces a pattern of neurotoxicity with a spectrum of severity ranging from trivial to life threatening. Patients stung by Centruroides scorpions develop a clinical syndrome which may require sedation with benzodiazepines and observation for 6 to 28 hours of intensive care monitoring. A safe therapy is necessary to halt the progression of symptoms early in the clinical course while avoiding the clinical deterioration that can occur en route to a tertiary facility. Alacramyn® is anticipated to be safer and more effective than the present standard of care, midazolam, and faster-acting thus eliminating the need to transport most rural patients and reducing hospitalization time.

开始日期2004-04-01

申办/合作机构

Instituto Bioclon SA de CV

[+2]

100 项与 Scorpion venoms 相关的临床结果

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100 项与 Scorpion venoms 相关的转化医学

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0 项与 Scorpion venoms 相关的专利（医药）

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项与 Scorpion venoms 相关的文献（医药）

2018-04-01·Neuropharmacology2区 · 医学

Voltage-gated sodium channel β subunits: The power outside the pore in brain development and disease

2区 · 医学

Review

作者: Hull, Jacob M ; Isom, Lori L

Voltage gated sodium channels (VGSCs) were first identified in terms of their role in the upstroke of the action potential. The underlying proteins were later identified as saxitoxin and scorpion toxin receptors consisting of α and β subunits. We now know that VGSCs are heterotrimeric complexes consisting of a single pore forming α subunit joined by two β subunits; a noncovalently linked β1 or β3 and a covalently linked β2 or β4 subunit. VGSC α subunits contain all the machinery necessary for channel cell surface expression, ion conduction, voltage sensing, gating, and inactivation, in one central, polytopic, transmembrane protein. VGSC β subunits are more than simple accessories to α subunits. In the more than two decades since the original cloning of β1, our knowledge of their roles in physiology and pathophysiology has expanded immensely. VGSC β subunits are multifunctional. They confer unique gating mechanisms, regulate cellular excitability, affect brain development, confer distinct channel pharmacology, and have functions that are independent of the α subunits. The vast array of functions of these proteins stems from their special station in the channelome: being the only known constituents that are cell adhesion and intra/extracellular signaling molecules in addition to being part of channel complexes. This functional trifecta and how it goes awry demonstrates the power outside the pore in ion channel signaling complexes, broadening the term channelopathy beyond defects in ion conduction. This article is part of the Special Issue entitled 'Channelopathies.'

2006-09-01·The FASEB Journal2区 · 生物学

Allosteric interactions between scorpion toxin receptor sites on voltage‐gated Na channels imply a novel role for weakly active components in arthropod venom

2区 · 生物学

Article

作者: Gordon, Dalia ; Cohen, Lior ; Lipstein, Noa

Scorpion beta and alpha-toxins modify the activation and inactivation of voltage-gated sodium channels. Although the two types of toxin bind at two distinct receptor sites on the same sodium channel, they exhibit synergic effects when coinjected into insects. To clarify the basis of this synergism we examined the mutual effects of alpha and beta toxin representatives in radio-ligand binding assays. We found positive allosteric interactions between receptor site-4 of the excitatory Bj-xtrIT and the depressant LqhIT2 beta toxins and receptor site-3 of the alpha toxin LqhalphaIT, on locust neuronal membranes. Unexpectedly, a nontoxic mutant Bj-xtrIT-E15R, which binds with high affinity to receptor site-4, was able to enhance LqhalphaIT binding and toxicity similarly to the unmodified Bj-xtrIT. This result indicates that mere binding of a nontoxic ligand to receptor site-4 ("silent binding") induces a conformational change that does not alter channel gating, but influences toxin binding at receptor site-3 leading to enhanced toxicity. This finding suggests a new functional role for weakly toxic polypeptides in that they enhance the effect of other active neurotoxins in the arthropod venom. Such silent binding may have also valuable implications in attempts to improve drug efficacy by combining potent drugs with nonactive allosteric enhancers.

2003-04-10·FEBS Letters3区 · 生物学

Allosteric interactions among pyrethroid, brevetoxin, and scorpion toxin receptors on insect sodium channels raise an alternative approach for insect control

3区 · 生物学

Article

作者: Michael Gurevitz ; Dalia Gordon ; Nicolas Gilles

Intensive pyrethroid use in insect control has led to resistance buildup among various pests. One alternative to battle this problem envisions the combined use of synergistically acting insecticidal compounds. Pyrethroids, scorpion α‐ and β‐toxins, and brevetoxins bind to distinct receptor sites on voltage‐gated sodium channels (NaChs) and modify their function. The binding affinity of scorpion α‐toxins to locust, but not rat‐brain NaChs, is allosterically increased by pyrethroids and by brevetoxin‐1. Brevetoxin‐1 also increases the binding of an excitatory β‐toxin to insect NaChs. These results reveal differences between insect and mammalian NaChs and may be exploited in new strategies of insect control.