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相关概念视频

Direct-Acting Cholinergic Agonists: Pharmacokinetics01:31

Direct-Acting Cholinergic Agonists: Pharmacokinetics

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Direct-acting cholinergic agonists, such as synthetic choline esters and naturally occurring alkaloids, exert their effects by enhancing the actions of acetylcholine and stimulating the parasympathetic nervous system. Synthetic choline esters share structural similarities with acetylcholine. For example, they have a positively charged quaternary ammonium or onium group, contributing to their hydrophilic characteristics. As a result, they are poorly absorbed in the body through oral...
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Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics01:11

Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics

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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...
444
Drug Delivery: Miscellaneous Routes01:22

Drug Delivery: Miscellaneous Routes

338
Drug delivery methods like oral inhalation, nasal sprays, transdermal patches, eye drops, intravitreal injection,  and rectal administration provide localized effects with reduced toxicity.
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs...
338
Cholinergic Antagonists: Pharmacokinetics01:24

Cholinergic Antagonists: Pharmacokinetics

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Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations,  while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and...
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Insulin Formulations: Types and Delivery01:27

Insulin Formulations: Types and Delivery

190
Insulin preparations are categorized by their duration of action into short-acting and long-acting types. Two strategies are used to modify insulin's absorption and pharmacokinetic profile: slowing the absorption post-subcutaneous injection, or altering human insulin's amino acid sequence or protein structure. These changes retain the insulin's ability to bind to the insulin receptor, but alter its behavior in solution or after injection.
Short-acting insulins are divided into...
190
Indirect-Acting Cholinergic Agonists: Pharmacokinetics01:22

Indirect-Acting Cholinergic Agonists: Pharmacokinetics

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Indirect-acting cholinergic agonists, or anticholinesterases, enhance the body's cholinergic activity by inhibiting acetylcholine's breakdown. They are categorized as reversible or irreversible agents based on their mechanism of action. They are further classified into short-acting, intermediate-acting, and long-acting agents based on their duration of action.
Reversible agents containing quaternary amines, such as neostigmine and edrophonium, are not easily absorbed orally because they...
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Author Spotlight: A Novel Protocol for Intracameral Injections to Enhance Precision in Rodent Ophthalmology
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阿尔布卡切尔对于长效疗法的治疗方法

Ji Hyun Rho1, Jae Hun Lee1, Inchan Kwon1

  • 1School of Materials Science and Engineering, Gwangju Institute of Science and Technology (GIST), Gwangju 61005, Republic of Korea.

ACS omega
|June 3, 2024
PubMed
概括

阿尔布卡切尔策略通过将它们与人血清白蛋白 (HSA) 结合,成功地延长了治疗性蛋白质的血清半衰期. 这种方法通过利用HSA来提高蛋白质的有效性.

科学领域:

  • 生物技术是生物技术.
  • 蛋白质工程是指蛋白质工程.
  • 药理学 药理学是指药理学的学科.

背景情况:

  • 治疗性蛋白质具有很高的选择性,但患有短血清半衰期,限制了它们的有效性.
  • 延长蛋白质半衰期的策略对于持续的治疗效果至关重要.
  • 由于Fc受体 (FcRn) 的循环,人类血清白蛋白 (HSA) 具有很长的内在半衰期.

研究的目的:

  • 推出AlbuCatcher,一种用于延长治疗性蛋白质血清半衰期的新型结合系统.
  • 为了证明AlbuCatcher对各种蛋白质疗法的普遍适用性.
  • 评估AlbuCatcher对蛋白质活性和药理动学的影响.

主要方法:

  • 开发了AlbuCatcher使用SpyCatcher与HSA结合.
  • 使用逆电子需求迪尔斯-阿尔德 (IEDDA) 反应用于特定地点的HSA结合.
  • 将SpyTag合到尿酸氧化酶 (Uox) 中,以创建用于与AlbuCatcher结合的Uox-ST.

主要成果:

  • 通过AlbuCatcher反应成功制备了HSA结合的Uox (Uox-HSA).
  • 实验室试验证实结合对Uox酶活性的影响微不足道.

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  • 用小鼠进行的药理动力学研究表明,Uox-HSA的半衰期从Uox-WT的2小时延长到~18小时.
  • 结论:

    • 阿尔布卡切尔策略有效地延长了治疗性蛋白质的血清半衰期.
    • 结合HSA的FcRn介导循环利用有助于延长半衰期.
    • 阿尔布卡切尔代表了一种增强治疗性蛋白质药理动学的有前途的方法.