Medicinal Chemistry

406 7 Nonmessenger Targets for Drug Action I Endogenous cellular structures 7.1 Cellular Structures: Relevant Anatomy and Physio ...

The cell membrane envelops the entire cell and is semipermeable. The aqueous interior of the cell has an ionic composition marke ...

The composition of the cell membrane varies from one anatomical location to another. For example, the cell membranes of neurons ...

large nucleoli and may even have more than one nucleolus. The cell nucleus is the site of the storage and replication of most of ...

form the inner, hydrophobic part of the lipid bilayer, which behaves as a liquid. Cholesterol serves to make the bilayer more ri ...

sterol in fungi. Amphotericin B binds to cell membrane ergosterol in the fungi, and the resulting drug–lipid complex produces le ...

7.3 Targeting Cell Membrane Structures: Protein Component The other major structural features of cell membranes are the proteins ...

connexons(one in each of the two adjoining cells); each connexon is composed of six homologous subunits, the connexin proteins. ...

the GABA-A ionophore channel, and the glycine receptor—the latter two both being Cl−channels—show about 50% homology, have close ...

The potassium channel, on the other hand, is blocked by both tetraethylammonium salts (7.3, TEA) and nonyl-triethylammonium (7.4 ...

GABA-A or NMDA channels, within the central nervous system (i.e., the brain). The term anesthesia may therefore be defined as a ...

esters typically have a shorter duration of action. This observation enables the drug designer to engineer, with insight, a comp ...

saxitoxin (7.2)). The interaction of the local anesthetic with the receptor protein is seemingly via a three-point binding inter ...

Regional nerve block anesthesia—injection of a small amount of local anesthetic into the tissue immediately surrounding a nerve ...

through the His–Purkinje system is coupled to mechanical contraction of the heart’s ventricular muscles. The electrical generati ...

ibutilide (7.24). Class IV compounds include traditional Ca^2 +channel blockers such as verapamil (7.25) and diltiazem (7.26). 7 ...

contains 100 billion neurons. When a neuron is injured it may either “hypofunction,” producing paralysis, or “hyperfunction,” pr ...

7.4.4.1 The Clinical–Molecular Interface: Epilepsy and Voltage-Gated Na+Channels Case History. “My seizures start without any wa ...

From a clinical perspective, some of these PCO classes have attracted initial attention. Diazoxide and minoxidil have been evalu ...

Clearly, Ca^2 + is an important regulator and mediator of endogenous molecular processes, both functionally and structurally. Th ...