Histamine acts by binding to specialized membrane proteins called histamine H 1 receptors. These receptors, found in specific cells, are integral membrane proteins that possess seven transmembrane a-helical regions. The amino terminus of the protein is extracellular, while the C-terminus is cytoplasmic. The binding of histamine to the extracellular portion of the H 1 receptor prompts a conformational change in the intracellular C-terminus region of the protein. This conformational change triggers numerous intracellular signaling events that stimulate the immune response in cells containing the receptor. There are numerous anti-histamine drugs available commercially. Some of the most popular are shown here side by side with histamine: CH2CH3 CH3 HO -NH Allegra histamine Claritin Propose a reasonable mode of action by which these antihistamines exert their activity. Include relevant details about the system of your own choosing.
Histamine acts by binding to specialized membrane proteins called histamine H 1 receptors. These receptors, found in specific cells, are integral membrane proteins that possess seven transmembrane a-helical regions. The amino terminus of the protein is extracellular, while the C-terminus is cytoplasmic. The binding of histamine to the extracellular portion of the H 1 receptor prompts a conformational change in the intracellular C-terminus region of the protein. This conformational change triggers numerous intracellular signaling events that stimulate the immune response in cells containing the receptor. There are numerous anti-histamine drugs available commercially. Some of the most popular are shown here side by side with histamine: CH2CH3 CH3 HO -NH Allegra histamine Claritin Propose a reasonable mode of action by which these antihistamines exert their activity. Include relevant details about the system of your own choosing.
Biochemistry
9th Edition
ISBN:9781319114671
Author:Lubert Stryer, Jeremy M. Berg, John L. Tymoczko, Gregory J. Gatto Jr.
Publisher:Lubert Stryer, Jeremy M. Berg, John L. Tymoczko, Gregory J. Gatto Jr.
Chapter1: Biochemistry: An Evolving Science
Section: Chapter Questions
Problem 1P
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
Transcribed Image Text:Histamine acts by binding to specialized membrane proteins called histamine H1 receptors. These receptors, found in specific cells, are integral membrane proteins that possess seven transmembrane a-helical regions. The amino terminus of the protein is extracellular, while the C-terminus is cytoplasmic. The binding of histamine to the extracellular portion of the H1 receptor prompts a conformational change in the intracellular C-terminus region of the protein. This conformational change triggers numerous intracellular signaling events that stimulate the immune response in cells containing the receptor.
There are numerous anti-histamine drugs available commercially. Some of the most popular are shown here side by side with histamine:
- **Histamine Structure:** A simple organic compound, consisting of an imidazole ring with an ethylamine chain.
- **Allegra (Fexofenadine) Structure:** A more complex structure featuring multiple ring systems, including a piperidine ring and a benzhydryl group, along with an ethyl ester and hydroxyl groups.
- **Claritin (Loratadine) Structure:** Characterized by a tricyclic framework with a characteristic carbamate group and additional ethyl and chlorine substituents.
**Prompt for Further Exploration:**
Propose a reasonable mode of action by which these antihistamines exert their activity. Include relevant details about the system of your own choosing.
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