Emedastine Difumarate is a potent, orally active, selective, and high-affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. It is an effective anti-allergic medication with a promising future.
I. Basic Information
Chemical Name: Emedastine Difumarate
CAS Number: 87233-62-3
Molecular Formula: C25H34N4O9
Molecular Weight: 534.56
II. Pharmacological Action
Emedastine Difumarate exerts its pharmacological effects by antagonizing histamine H1 receptors with high potency and selectivity.
It has a high affinity (Ki = 1.3 nM) for histamine H1 receptors, while showing lower affinity (Ki values of 49067 nM and 12430 nM, respectively) for histamine H2 and H3 receptors.
III. Indications and Uses
Emedastine Difumarate is used in the treatment of various allergic conditions, including allergic rhinitis, allergic skin disorders, and allergic conjunctivitis.
As an eye drop (e.g., Emedastine Difumarate Ophthalmic Solution), it is primarily used for the temporary relief of the signs and symptoms of allergic conjunctivitis.
