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Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics01:11

Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics

All neuromuscular blocking agents are injected intravenously because they are poorly absorbed from the GI tract. Rapid onset is achieved with intravenous administration, although absorption is also adequate from an intramuscular injection. Since these agents are highly ionized, they do not readily penetrate cell membranes or cross the blood-brain barrier.
Instead, they are transported by the blood to different tissues. Muscles with a greater blood supply (arteries) and blood flow receive more...
Depolarizing Blockers: Mechanism of Action01:28

Depolarizing Blockers: Mechanism of Action

Depolarizing blockers act on skeletal muscle fibers' membranes and induce their depolarization. Most depolarizing blockers have two quaternary N+ atoms that bind the nicotinic acetylcholine receptors and cause neuromuscular blockade within minutes.
Succinylcholine is the most commonly used depolarizing blocker. Chemically, it constitutes two molecules of acetylcholine joined together by an acetate methyl group. They act on the receptors in the same way as acetylcholine. Because succinylcholine...
Depolarizing Blockers: Pharmocokinetics01:19

Depolarizing Blockers: Pharmocokinetics

Depolarizing blockers are administered through intravenous injection. Succinylcholine is the most common choice of depolarizing blockers in emergency clinical practices. Although they have a rapid onset, they readily diffuse away from the motor end plate into the extracellular fluid. They are metabolized by enzymes such as liver butyrylcholinesterase and plasma pseudocholinesterases. This produces a short duration of action, typically 5-10 minutes long, unlike nondepolarizing blockers, which...
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
Drug Product Stability01:16

Drug Product Stability

The long-term stability of drug products is critical to ensuring their quality, safety, and effectiveness over time. Stability directly influences a product's ability to maintain its intended characteristics, ensuring it performs as expected during its intended shelf life. Key attributes such as drug potency, impurities, dissolution, and other physicochemical measures of performance are tested to assess stability. These parameters indicate how well the product retains its quality over time and...
Pharmaceutical Alternatives: Stability-Related Therapeutic Nonequivalence01:22

Pharmaceutical Alternatives: Stability-Related Therapeutic Nonequivalence

Generic intravenous (IV) drugs are considered bioequivalent to their branded counterparts due to their 100% bioavailability upon administration. However, variations in stability among different drug products can significantly influence their therapeutic performance, even if they are pharmaceutically equivalent.Cefuroxime, a prophylactic antimicrobial, is often used as a single-dose IV injection for patients undergoing coronary artery bypass grafting surgery. A 3 g dose typically provides...

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Updated: Jul 8, 2026

Thermostabilization, Expression, Purification, and Crystallization of the Human Serotonin Transporter Bound to S-citalopram
12:21

Thermostabilization, Expression, Purification, and Crystallization of the Human Serotonin Transporter Bound to S-citalopram

Published on: November 27, 2016

孤立したベータシートのエントロピー安定化.

Philippe Dugourd1, Rodolphe Antoine, Gary Breaux

  • 1Laboratoire de Spectrométrie Ionique et Moléculaire, UMR No. 5579, CNRS et Université Lyon 1, 43 bd du 11 novembre 1918, 69622 Villeurbanne Cedex, France.

Journal of the American Chemical Society
|March 31, 2005
PubMed
まとめ

10個以上のアラニン単位を有する溶解していないアラニン基ペプチド (Ac-WA(n) -NH(2) は,室温でベータシート構造を採用する. ガス相におけるペプチド構造は主に電荷の位置によって制御されるが,アラニンはそうではない.

科学分野:

  • バイオフィジックス 生物物理学
  • コンピューティング・ケミストリー
  • ペプチド科学 ペプチド科学

背景:

  • アラニンベースのペプチドは,生体物理学の研究における基本的なモデルである.
  • 溶液中のペプチド構成は,ガス相または固体構造と大きく異なる.
  • 以前の研究では,電荷の位置がガス相ペプチド構造に影響することを示しています.

研究 の 目的:

  • 溶解されていないアラニン基ペプチドのガス相構成を調べる.
  • ペプチドの長さと電荷が二次構造に及ぼす影響を判断する.
  • アラニン豊富な配列の溶液相とガス相の構造的傾向を比較する.

主な方法:

  • ペプチド構造を検知するために,温度依存の電気偏移測定を用いた.
  • データを解釈するために,並行テンプリングアルゴリズムを備えたモンテカルロシミュレーションを使用した.
  • 様々なアラニン長さ (n=3, 5, 10, 13, 15) を有するアセチル化されたトリプトファン-アラニンペプチド (Ac-WA(n) -NH(2) を研究した.

主要な成果:

  • n > 10の溶解されていないAc-WA(n) -NH(2) ペプチドは,室温でベータシート形状を主に採用する.
  • これは,溶液中のアラニンの高いヘリックス傾向と対照的です.

さらに関連する動画

How to Stabilize Protein: Stability Screens for Thermal Shift Assays and Nano Differential Scanning Fluorimetry in the Virus-X Project
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How to Stabilize Protein: Stability Screens for Thermal Shift Assays and Nano Differential Scanning Fluorimetry in the Virus-X Project

Published on: February 11, 2019

Isolation and Analysis of Traceable and Functionalized Extracellular Vesicles from the Plasma and Solid Tissues
09:57

Isolation and Analysis of Traceable and Functionalized Extracellular Vesicles from the Plasma and Solid Tissues

Published on: October 17, 2022

関連する実験動画

Last Updated: Jul 8, 2026

Thermostabilization, Expression, Purification, and Crystallization of the Human Serotonin Transporter Bound to S-citalopram
12:21

Thermostabilization, Expression, Purification, and Crystallization of the Human Serotonin Transporter Bound to S-citalopram

Published on: November 27, 2016

How to Stabilize Protein: Stability Screens for Thermal Shift Assays and Nano Differential Scanning Fluorimetry in the Virus-X Project
07:22

How to Stabilize Protein: Stability Screens for Thermal Shift Assays and Nano Differential Scanning Fluorimetry in the Virus-X Project

Published on: February 11, 2019

Isolation and Analysis of Traceable and Functionalized Extracellular Vesicles from the Plasma and Solid Tissues
09:57

Isolation and Analysis of Traceable and Functionalized Extracellular Vesicles from the Plasma and Solid Tissues

Published on: October 17, 2022

  • ペプチドの構造は,以前に観察したように,電荷の位置に非常に敏感です.
  • 結論:

    • アラニンベースのペプチドのガス相二次構造は,固有のアミノ酸の傾向によってのみ決定されるわけではありません.
    • ペプチドの長さと溶媒の欠如は,安定した形状を決定する上で重要な役割を果たします.
    • 充電局所化は,ガス相におけるこれらのペプチドの全体的な構造を制御する支配的な要因です.