Heteroatoms as well as heterocyclic scaffolds are frequently present as the common cores in a plethora of active pharmaceuticals natural products. Statistically, more than 85% of all biologically active compounds are heterocycles or comprise a heterocycle and most frequently, nitrogen heterocycles as a backbone in their complex structures. These facts disclose and emphasize the vital role of heterocycles in modern drug design and drug discovery. In this review, we try to present a comprehensive overview of top prescribed drugs containing nitrogen heterocycles, describing their pharmacological properties, medical applications and their selected synthetic pathways. It is worth mentioning that the reported examples are actually limited to current top selling drugs, being or containing N-heterocycles and their synthetic information has been extracted from both scientific journals and the wider patent literature.

/pdf/prescribed-drugs-containing-nitrogen-heterocycles-an-31vxbjpp0q.pdf

Prescribed drugs containing nitrogen heterocycles: an overview

α-Adrenoceptor subclassification

Clonidine binds to imidazole binding sites as well as α2-adrenoceptors in the ventrolateral medulla

[3H]WB-4101 and p-[3H]aminoclonidine were used for light microscopic autoradiographic localization of alpha 1 and alpha 2 adrenergic receptors, respectively, in the rat brain. The binding of these ligands to slide-mounted tissue sections had all of the characteristics associated with alpha 1 and alpha 2 receptors. It was saturable with appropriate kinetic constants and was blocked only by other alpha-adrenergic drugs with the appropriate potency. Autoradiographic studies revealed a distribution of alpha-adrenergic receptors throughout the nervous system. Certain areas had elevated levels. These included parts of the olfactory bulb and nucleus, parts of the cerebral cortex and dentate gyrus, the more medial portions of the hypothalamus and thalamus, the locus ceruleus and nucleus tractus solitarii, and parts of the spinal cord. In certain areas, the distribution of alpha 1 and alpha 2 receptors was markedly different. These results provide some rational basis for the observed actions of alpha-adrenergic drugs on the central nervous system. For example, the finding of high densities of alpha 2 receptors in the nucleus tractus solitarii is most likely related to its antihypertensive action. The observed codistribution of alpha 2 receptors with opiate receptors would provide an explanation of the observation that alpha 2 agonists block opiate withdrawal. The results are also discussed in relationship to the anatomy of catecholamine systems in the brain.

https://www.pnas.org/content/pnas/77/3/1696.full.pdf

Noradrenergic alpha 1 and alpha 2 receptors: light microscopic autoradiographic localization

Xylazine--a review of its pharmacology and use in veterinary medicine.

Central α-adrenergic systems as targets for hypotensive drugs

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Central α-adrenergic systems as targets for hypotensive drugs