H1-antagonists, also known as H1 receptor antagonists or antihistamines, are a class of drugs that block the action of histamine at the H1 receptors. The body produces histamine, a natural substance that plays a key role in various physiological processes, especially in immune responses and allergic reactions. Ethylene diamine derivatives Ethylene diamine derivatives, characterized by … Read more
1. H1-Antagonists with classical structures According to the chemical features, they are further classified as follows: a. Ethylene diamine derivatives b. Amino alkyl ether analogues c. Cyclic basic chain analogues d. Mono amino propyl analogues d. i. Saturated analogues d. ii. Unsaturated analogues e. Tricyclic ring system or Phenothiazine derivatives f. Dibenzocyclo heptane’s g. Miscellaneous … Read more
The structure-activity relationship (SAR) for H1 receptor antagonists, commonly known as antihistamines, involves understanding how the chemical structure of a compound influences its pharmacological activity in blocking the H1 receptors. Here are some key aspects of the SAR for H1 receptor antagonists: 1. Aryl groups The diaryl substitution is essential for significant H1 affinity. It is … Read more
INTRODUCTION Histamine, [2-(imidazol-4-y1) ethylamine], which is biosynthesized by decarboxylation of the essential amino acid histidine, is found in all organs and tissues of the human body. Reaction: Histamine is stored within the secretory granules of mast cells, maintaining a pH of 5.5. It exists in a positively charged state and forms ionic complexes with the … Read more
