Receptors interaction with drugs

The first four chapters and Chapter 6 are connected with 3D molecular descriptors and their uses for QSAR and molecular similarity studies associated with molecular modeling of agonist-receptor interactions, with drug design, and with the discovery of new lead compounds for various types of biological activities. 

In addition to sequence structural information on molecules themselves, these molecules have been categorized and classified according to their functions and interactions with drugs or other molecules. For example, some Web sites and databases can be used for studying such specific genetic molecules, including receptors and transporters. 

Murphy, D.L., Andrews, A.M., Wichems, C.H., Li, Q., Tohda, M., and Greenberg, B. (1998) Brain serotonin neurotransmission an overview and update with an emphasis on serotonin subsystem heterogeneity, multiple receptors, interactions with other neurotransmitter systems, and consequent implications for understanding the actions of serotonergic drugs. J Clin Psychiatry 59 5uppl 15 4-12. 

Hypericum has been found to also interact with drugs metabolized via other pathways. For example, it decreases serum levels of digoxin, which is metabolized via the P-glycoprotein drug transporter, and reduces levels of theophylline and warfarin, which are metabolized via CYP1A2 and CYP2C9 pathways, respectively. It is possible that St. John s wort might also induce those enzymes via the steroid X receptor (Wentworth et ah, 2000). 

Admittedly, the separation of enantiomers is often difficult and expensive. However, now that we are in the 21st century, the need for optically active drugs capable of stereospecific interactions with drug receptors is a recognized prerequisite in drug design. 

Until now we have considered receptor interactions and drug effects in terms of equations and concentration-effect curves. We must also understand the molecular mechanisms by which a drug acts. Such understanding allows us to ask basic questions with important clinical implications ... 

Muscarinic cholinergic receptors and their interactions with drugs, 18, 432... 

Drug-receptor interactions may quantitatively differ among rapidly converting multiple receptor states that are induced by agonist binding. While most studies commonly focus on analysis of ligand-receptor interactions and cellular responses under presumed steady-state conditions, experimental techniques available for the quantitative analysis of drug-receptor interactions with transient receptor conformational... 

Muscarinic cholinergic receptors and their interactions with drugs. 18. 432 Muscarine receptors in peripheral and central nervous systems. 2. 143... 

Interaction with enzymes usually involves inhibition, but enzyme induction also has its uses, or can occur unintentionally. Interactions generally occur by binding at the active site of the enzyme (where the substrate binds), in a very similar manner to receptor binding - the comments below, concerning receptors, can equally apply to enzyme interactions with drugs. 

It is now widely accepted that the receptors that interact with drugs to produce a drug reaction are largely protein in nature. Thus the two distances between helical turns and peptide bonds assume potential significance in the mechanism of drug action at the molecular level. It is possibly more than coincidence that a considerable number of drugs have functional groups believed to be involved in receptor complexation that are separated by dis-... 

Rimonabant is the first endocannabinoid-CB [1] blocking drug in the treatment of obesity. The CBl receptor is widely distributed in CNS and these receptors interact with several pathways involved in appetite regulation (e.g. ghrehn and leptin pathways). Rimonabant may, however, also have... 

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