Introduction Clemastine fumarate is a white crystalline powder, very slightly soluble in water slightly soluble in alcohol, and methanol. It has two chiral centers, each of which is (R) absolute configuration. A comparison of the activities of the antipodes indicates that the asymmetric center close to the side chain of nitrogen is of lesser importance … Read more
Carbinoxamine is an antihistamine that is commonly used to alleviate symptoms associated with allergies, such as sneezing, itching, and runny nose. It belongs to the first-generation antihistamine class and works by blocking the effects of histamine at the H1 receptors. Structure Synthesis Mechanism of action Uses: Side Effects: Formulation: Carbinoxamine is available in various formulations, … Read more
Doxylamine, in the form of Decapryn Succinate, is an antihistamine with sedative properties. Commonly used for occasional sleeplessness, it is found in some over-the-counter sleep aids and allergy medications. Side effects may include drowsiness, dry mouth, and blurred vision. Structure Synthesis Mechanism of action: Doxylamine exerts its antihistamine effects by antagonizing H1 receptors. By blocking … Read more
Bromodiphenhydramine is a diphenhydramine derivative, an antihistamine used to treat allergy symptoms. As the name suggests, Bromodiphenhydramine contains a bromine atom in its structure. Adding bromine is a chemical modification intended to alter the properties or enhance the effects of the original diphenhydramine compound. Structure Synthesis Mechanism of action Bromodiphenhydramine competes with free histamine for … Read more
Dimenhydrinate is an antihistamine medication known for its efficacy in alleviating allergic symptoms. Notable for its H1 receptor-blocking action, it provides relief from conditions such as itching and runny nose. Moreover, dimenhydrinate’s central nervous system depression induces drowsiness, making it useful for motion sickness and as a sleep aid. With additional antiemetic and antimuscarinic properties, … Read more
Aminoalkyl ether analogs refer to chemical compounds that share a structural similarity with aminoalkyl ethers. These analogs typically involve the substitution of certain functional groups or moieties while maintaining the basic aminoalkyl ether framework. The term “aminoalkyl ether” indicates the presence of an amino group (-NH2) and an ether group (-O-) in the molecular structure. … Read more
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
