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Ligands, and Drugs

Figure 14.8. Sites of action of endogenous ligands and drugs that modulate the action of excitatory amino acids on the NMDA receptor. Recent evidence shows that glutamate (Glut) and possibly other excitatory amino acids released from presynaptic terminals activate the NMDA receptor site on postsynaptic membranes, resulting in the opening of the Na+/Ca++ channels. Glycine acts on a strychnine-insensitive receptor while polyamines (e.g. spermine and spermidine) also have a modulatory role. Conversely Zn++ and Mg++ and drugs like phencyclidine (PCP) block the ion channel by acting at various sites on the NMDA receptor complex or... Figure 14.8. Sites of action of endogenous ligands and drugs that modulate the action of excitatory amino acids on the NMDA receptor. Recent evidence shows that glutamate (Glut) and possibly other excitatory amino acids released from presynaptic terminals activate the NMDA receptor site on postsynaptic membranes, resulting in the opening of the Na+/Ca++ channels. Glycine acts on a strychnine-insensitive receptor while polyamines (e.g. spermine and spermidine) also have a modulatory role. Conversely Zn++ and Mg++ and drugs like phencyclidine (PCP) block the ion channel by acting at various sites on the NMDA receptor complex or...
Halazy, S. (1999) G-protein coupled receptors bivalent ligands and drug design. Expert Opin. Ther. Pat. 9, 431 46. [Pg.41]

Application and limitations of X-ray crystallographic data in structure-based ligand and drug design for screening 03AG(E)2718. [Pg.177]

Fig. 3.1 Schematic representation of the series of biochemical steps leading from ligand-receptor interaction to the cellular and physiological responses. LI, L2 and D stand for ligand and drug, respectively. R1 and R2 represent specific membrane receptors that recognize Li and L2. El — n are effector proteins, generally enzymes, modulated by receptor activation or by drugs acting as inhibitors. S is a specific substrate. Fig. 3.1 Schematic representation of the series of biochemical steps leading from ligand-receptor interaction to the cellular and physiological responses. LI, L2 and D stand for ligand and drug, respectively. R1 and R2 represent specific membrane receptors that recognize Li and L2. El — n are effector proteins, generally enzymes, modulated by receptor activation or by drugs acting as inhibitors. S is a specific substrate.
The isomers differ quantitatively in their activities, one enantiomer being more active then the other but facilitating the same overall response. In the extreme situation one enantiomer may exhibit zero biological activity. The majority of chiral ligands and drugs fall into this category. [Pg.462]

Gresh N (2006) Development, validation, and applications of anisotropic polarizable molecular mechanics to study ligand and drug-receptor interactions. Curr Pharm Des 12(17) 2121-2158. doi 10.2174/138161206777585256... [Pg.271]

Davis, A.M., Teague, S.J., and Kleywegt, G.J. 2003. Application and limitations of x-ray crystallographic data in structure-based ligand and drug design. Angew. Chem., 42, 2718-2736. [Pg.86]


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