General structural features of 1st gen. H1 antagonist. Structure moa, uses of chlorpheniramine maleate, promethazine hydrochloride, doxylamine succinate.

General Structure of H1 Antagonists

  1. Aryl group: The diaryl substitution is essential for significant H1-receptor affinity. The optimal antihistaminic activity depends upon the co-planarity of two aryl substitutions.
  2. Nature of ‘X’: The X-connecting moiety of H1-antihistamines may be a simple carbon chain or saturated carbon-oxygen moiety, which serves as a spacer group for the required pharmacophore.
  3. Alkyl chain (The carbon chain): The carbon chain consists of two or three atoms in H1-antihistamines.
  4. Terminal Nitrogen: This is a basic, terminal amine functional group. Contains small alkyl substituting. 

Promethazine 

USES - Allergic reaction, Motion sickness
 Insomnia, Cough, Nausea 

chlorpheniramine maleate

USES- symptoms of allergic reactions; over-the-counter products for cold; depression, nausea and vomiting, motion sickness, and vertigo.


doxylamine succinate


USES - Allergic reaction, Motion sickness; Insomnia, Cough, Nausea 

MOA - 



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