Hans Bruner Osborne

12.1.1 Synaptic Processes and 12.2 Receptor Structure and 12.2.1 G Protein-Coupled 12.2.2 Ligand-Gated Ion Channel 12.2.2.1 The Cys-Loop Receptor 12.2.2.2 The Ionotropic Glutamate Receptor 12.2.3 Tyrosine Kinase 12.2.4 Nuclear 12.3 Receptor 12.3.1 Recombinant versus in Situ 12.3.2 Binding versus Functional 12.3.3 Partial and Full 12.3.4 Antagonists 12.3.5 Constitutively Active Receptors and Inverse 12.3.6 Allosteric 12.3.6.1 Negative Allosteric Modulators (Noncompetitive Antagonists) 203...

XX x

Fusidic Acid Cream Mechanism Action

FIGURE 24.12 Mechanism of antiviral action of acyclovir (ACV). ACV targets viral DNA polymerases, such as the herpesvirus (HSV) DNA polymerase. Before it can interact with viral DNA synthesis, it needs to be phosphorylated intracellularly, in three steps, to the triphosphate form. The first phosphorylation step is ensured by the HSV-encoded thymidine kinase (TK), and is therefore confined to virus-infected cells. (After De Clercq, E., Nat. Rev. Drug Discov., 1, 13, 2002.) FIGURE 24.12 Mechanism...

Copper Silver and Gold

Copper and iron constitute the most important redox active transition metals in bioinorganic chemistry, and they seem to complement each other. Both copper and iron proteins are involved in oxygen transport and charge transfer. But while the iron containing proteins and enzymes always are found intracellularly, copper proteins and enzymes mainly operate outside the cells. In humans most copper is found in the brain, the heart, and the liver. The high metabolic rate of these organs requires...

Iwan de Esch Henk Timmerman and Rob Leurs

17.2 The Histamine H1 Receptor Molecular Aspects and Selective 17.2.1 Molecular Aspects of the Histamine Hj Receptor 17.2.2 H1 Receptor 17.2.3 H1 Receptor 17.2.4 Therapeutic Use of H1 Receptor 17.3 The Histamine H2 Receptor Molecular Aspects and Selective 17.3.1 Molecular Aspects of the Histamine H2 Receptor 17.3.2 H2 Receptor 17.3.3 H2 Receptor 17.3.4 Therapeutic Use of H2 Receptor 17.4 The Histamine H3 Receptor Molecular Aspects and Selective 17.4.1 Molecular Aspects of the Histamine H3...

Bjarke Ebert and Keith A Wafford

20.2 Sleep 20.3 Pharmacological Modulation of the Sleep 20.3.1 Induction and Maintenance of 20.3.1.1 Benzodiazepines and Benzodiazepine Receptor Agonists 332 20.3.2 Modulating Slow Wave Sleep and Slow Wave 20.3.2.1 GABAa Receptor 20.3.2.2 5-HT2A 20.3.4 Melatonin and Melatonergic 20.4 Concluding Further Problems with sleep (falling asleep, maintaining sleep, waking up early, or not feeling refreshed after sleep) can occur in some patients as a disease in its own right and in other patients as a...

Rasmus P Clausen and Harald S Hansen

Tetrahydrocannabinol Mechanism Action

19.1 Opioid 19.1.1 Opioid Receptor Subtypes and Effector 19.1.2 Endogenous Opioid Receptor 19.1.3 Nonendogenous Opioid Receptor 19.1.4 Therapeutic Applications and 19.2 Cannabinoid 19.2.1 Endocannabinoid 19.2.2 Cannabinoid Receptor 19.2.3 Cannabinoid Receptor 19.2.4 Other Cannabinoid 19.2.5 Therapeutic Use and 19.2.6 FAAH-Inhibitors and Anandamide Uptake 19.2.7 CBj-Receptor 19.2.8 CB2-Receptor 19.2.9 Diacylglycerol Lipase 19.2.10 Monoacylglycerol Lipase Further Presently she cast a drug into...

Fastacting Insulins

Biostructure-based drug design is not limited to design of low-molecular weight compounds based on knowledge of the structure of their biological targets. In the following text we are presenting an example on biostructure-based design of macromolecular drug molecules, i.e., insulin analogs. FIGURE 2.11 Structures of the ligand-binding core of the ionotropic glutamate receptor GluR2. (A) The open, unbound form of GluR2 (pdb-code 1FTO). (B) The NeuroSearch compound NS1209 stabilizes GluR2 in the...

Seren B Christensen

Amphotericin Cancer Cell Membrane

21.2 Infections Caused by Helminthic 21.3 Infections Caused by Protozoan Parasites Other Than 21.5 Drugs against 21.5.1 Drugs Targeting Hemozoin 21.5.1.1 21.5.2 Drugs Targeting a Ca2+ Pump of Plasmodium 21.5.3 Drugs Targeting 21.5.4 Drugs Targeting Mitochondrial 21.5.4.1 21.5.5 Drugs with Nonestablished 21.5.6 Drugs Targeting Folate 21.6.1 Chloroquine 21.6.2 4-Quinolinemethanol 21.6.3 Antifolate 21.7 Concluding Further Infections including parasitic diseases account for approximately one-third...

What Is Fcyiiib

FIGURE 22.4 This image represents the polypeptide chain structure of a molecule of IgG. The numbers indicate the number of amino acids. In the actual molecule, the chains are folded so that each cysteine is brought close to the partner with which it forms a disulfide (S-S) bridge. FIGURE 22.4 This image represents the polypeptide chain structure of a molecule of IgG. The numbers indicate the number of amino acids. In the actual molecule, the chains are folded so that each cysteine is brought...

Claus J Loland and Ulrik Gether

14.2 Neurotransmitter Transporters Belonging to the SLC6 14.2.1 Structures and Mechanisms of SLC6 14.2.2 The Binding Sites for Na+ and Cl- Importance in Substrate Binding and 14.2.3 Substrate Specificity and Binding Sites in SLC6 Neurotransmitter 14.3 Drugs Targeting Biogenic Amine Transporters Specificity, Use, and Molecular Mechanisms of 14.3.1 Cocaine, Benztropine, and Other Tropane Class 14.3.2 Amphetamine and Other Nonendogenous 14.3.4 Other Biogenic Amine Transporter 14.4 Inhibitors of...

H2NOX

Vigabatrin Mechanism

Vigabatrin FIGURE 15.2 Structures of some GABA-AT inhibitors, compound 15.6 being inactive. (Figure 15.2), a suicide inhibitor for the enzyme GABA-aminotransferase (GABA-AT) responsible for GABA degradation, is used clinically as an anticonvulsant. Elevation in extracellular GABA levels by the inhibition of the reuptake of GABA is effected by Tiagabine (15.20) (refer to Figure 15.4) marketed for the treatment of epilepsy and in preclinical studies for treatment of anxiety and insomnia. The...

Structure Of Cah2edta

Ethylenediaminetetraacetic acid (EDTA) and its analogues are all excellent chelates sequestering most metal ions, but for the same reason they are also not selective. EDTA coordinates preferentially to hard metal ions (Section 10.4.2) and due to the large chelate effect, quite stable complexes are formed. Since EDTA is inadequately absorbed only from the gastrointestinal tract, it is usually administered by intravenous injections. But due to the low degree of selectivity the hazard of...