Medicinal Chemistry

Antiarrythmics, regulating the timing of heart muscle contraction and thus being useful in the treatment of heart rhythm irregu ...

three positive charges out of the cell for each Ca^2 +; the resulting negative inside charge of the resting cell therefore favou ...

The 1,4-dihydropyridines are the best studied Ca2+channel antagonists. A number of analogs within this series have been develope ...

A substituted phenyl ring at the C4 position optimizes activity; substitution with heteroaromatic rings (e.g., pyridine) produc ...

One final anecdote involving 1,4-DHP Ca2+channel blockers concerns their role in the discovery that grapefruit juice can markedl ...

with neurobehavioral deterioration in a variety of neuropsychological measures in post-traumatic epilepsy patients. Some would a ...

brain structures. The macroscopic features of these alterations include fibrous gliosis (i.e., “brain scarring”) with cellular s ...

7.6 TARGETING CELL MEMBRANE PROTEINS: TRANSMEMBRANE TRANSPORTER PROTEINS The voltage-gated and ligand-gated ion channels enable ...

7.6.1 The Clinical–Molecular Interface: Congestive Heart Failure and the Na+/K+ATPase Transporter Protein Congestive heart failu ...

excitability of the cell membrane. Since membrane excitability is crucial both to the spread of electrical activity throughout t ...

above, the cardiac glycosides are conformationally flexible molecules. The two regions of maximal conformational flexibility are ...

The cardiac glycosides that are employed clinically include digoxin (7.48), digitoxin (7.49), lanatoside (7.50), ouabain, and de ...

It should be emphasized that this narrow therapeutic margin is directly related to the mechanism of action which involves inhibi ...

Cardiac glycosides are the time-honored treatment for CHF, having been used for centuries. Nonetheless, since the administration ...

play a role in connective tissue diseases such as Sjogren’s syndrome and systemic lupus erythmatosus. The cytoplasm also contain ...

7.8 Targeting Cell Nucleus Structures The final nonmessenger cellular target for drug design is the cell nucleus—the storage sit ...

The nucleus of every human cell possesses 46 chromosomes (23 pairs), each chromosome consisting of one large DNA molecule. Each ...

to the control of cellular protein synthesis, drug design that targets nucleic acids should be reserved for major pathologies su ...

444 MEDICINAL CHEMISTRY through its amino groups. Above (and below) this intercalated ethidium molecule lies another one, which ...

Actinomycin Antitumor Antibiotics. Actinomycin D (7.56), produced by the fungus Actinomyces antibioticus, is an effective tumor- ...