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Chemistry

The hydroxyl group of aliskiren forms hydrogen bonds with both oxygen atoms of Asp32. ​ The amine group forms hydrogen bonds with Gly217's carboxylic acid group and Asp32's oxygen atom. ​ The aromatic ring's methoxy group fills the S3 pocket, potentially forming a hydrogen bond with Tyr14's secondary amine. ​ Aliskiren’s amide group forms a hydrogen bond with Ser76's secondary amine.​ Additionally, aliskiren selectively binds to the S3sp sub-pocket, contributing to its specificity as a renin inhibitor. ​ The binding is stabilized by these hydrogen bonds, showcasing the specificity and potency of aliskiren as a renin inhibitor. ​ Angeliki Giorgalli ( talk) 16:06, 25 February 2024 (UTC) reply

Basic Pharmacokinetics

Aliskiren, a hydrophilic renin inhibitor (logP= 2.45), displays exceptional selectivity and high aqueous solubility(>350 mg/ml), with favourable pharmacokinetics supporting once-daily dosing. ​ Metabolism occurs via CYP3A4, and despite low oral bioavailability (2.5%), its extensive tissue uptake and limited interactions make it a promising antihypertensive drug. (Vd= 135 L) ​ Aliskiren’s main route of elimination is via faeces, supported by a study which detected radio-labeled aliskiren showing more than 80% was found in faeces. Angeliki Giorgalli ( talk) 16:08, 25 February 2024 (UTC) reply

From Wikipedia, the free encyclopedia

External links modified

Hello fellow Wikipedians,

I have just modified one external link on Aliskiren. Please take a moment to review my edit. If you have any questions, or need the bot to ignore the links, or the page altogether, please visit this simple FaQ for additional information. I made the following changes:

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This message was posted before February 2018. After February 2018, "External links modified" talk page sections are no longer generated or monitored by InternetArchiveBot. No special action is required regarding these talk page notices, other than regular verification using the archive tool instructions below. Editors have permission to delete these "External links modified" talk page sections if they want to de-clutter talk pages, but see the RfC before doing mass systematic removals. This message is updated dynamically through the template {{ source check}} (last update: 18 January 2022).

  • If you have discovered URLs which were erroneously considered dead by the bot, you can report them with this tool.
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Cheers.— InternetArchiveBot ( Report bug) 12:18, 21 September 2017 (UTC) reply

Chemistry

The hydroxyl group of aliskiren forms hydrogen bonds with both oxygen atoms of Asp32. ​ The amine group forms hydrogen bonds with Gly217's carboxylic acid group and Asp32's oxygen atom. ​ The aromatic ring's methoxy group fills the S3 pocket, potentially forming a hydrogen bond with Tyr14's secondary amine. ​ Aliskiren’s amide group forms a hydrogen bond with Ser76's secondary amine.​ Additionally, aliskiren selectively binds to the S3sp sub-pocket, contributing to its specificity as a renin inhibitor. ​ The binding is stabilized by these hydrogen bonds, showcasing the specificity and potency of aliskiren as a renin inhibitor. ​ Angeliki Giorgalli ( talk) 16:06, 25 February 2024 (UTC) reply

Basic Pharmacokinetics

Aliskiren, a hydrophilic renin inhibitor (logP= 2.45), displays exceptional selectivity and high aqueous solubility(>350 mg/ml), with favourable pharmacokinetics supporting once-daily dosing. ​ Metabolism occurs via CYP3A4, and despite low oral bioavailability (2.5%), its extensive tissue uptake and limited interactions make it a promising antihypertensive drug. (Vd= 135 L) ​ Aliskiren’s main route of elimination is via faeces, supported by a study which detected radio-labeled aliskiren showing more than 80% was found in faeces. Angeliki Giorgalli ( talk) 16:08, 25 February 2024 (UTC) reply


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