Histamine receptor antagonists pharmacological properties

HiSTAMiNE RECEPTOR AGONiSTS act at one or more of the three receptor types that have been defined - Hj, H2 and Hj. Histamine itself can act at any of these sites, which have a variety of contrasting properties. The basic properties of these will be described, then followed by a description of the pharmacology of histamine. Antagonists at these receptors are described under separate headings see HISTAMINE Hi-RECEPTOR ANTAGONISTS HISTAMINE Hj-RECEPTOR... 

Antagonists - Recent structure-activity studies of Hj -receptor antihistamines have been concerned with stereochemical aspects, partition characteristics, pattern recognition, affinity contributions to activity and association phenomena. The subject has also been reviewed recently. Undoubtedly, the main focus of attention has been on the H2 receptor histamine antagonists. Three compounds have been widely studied, viz. burimamide (13b), metiamide (13c) and cimetidine (13d), and their pharmacological properties summarized. 3 Their discovery and development at SK F was the culmination of a research programme initiated in 1964. The search for an antagonist and some of the medicinal chemical approaches used in the structure-activity analysis have been outlined in several articles. Concurrently, other researchers had sought... 

Fox GB, Esbenshade TA, Pan JB, et al. Pharmacological properties of ABT-239 [4-(2- 2-[(2R)-2-methylpyrrolidinyl]ethyl -benzofuran-5-yl)benzonitrile] II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist. J Pharmacol Exp Ther 2005 313 176-190. 

The indolizine s)mthetic derivatives also deserve special attention because of their pharmacological properties such as antibacterial, anti-inflammatory, antiviral and antileishmanial, analgesic and antitumor, antioxidant activities, aromatase inhibition, calcium entry blocking, histamine H3 receptor antagonist, and physicochemical properties such as strong fluorescence [6, 7],... 

---