Medicinal Chemistry
Several nonsedative H 1 inhibitors have been marketed—for example, astemizole (4.149) and terfenadine (4.150). They are quite po ...
absorbed orally. The addition of a 4-methyl group further improved binding to the H 2 receptor. Introduction of the electron-wit ...
been “eaten through,” exposing the inner submucosal connective tissue layer. This mucosal damage is promoted by Helicobacter pyl ...
also remember that drugs designed to target CNS receptors can have systemic side effects and that drugs targeting systemic probl ...
indications. Antihistamines are usually the first drugs used to treat allergic reactions. They are very effective at reducing th ...
γ-Aminobutyric acid can be deactivated and recycled by the transamination reaction withα-ketoglutarate to yield glutamate. This ...
4.7.3 GABA Receptors: Presynaptic Drug Effects Presynaptic drug effects can interfere with the metabolism, storage, release, and ...
It is an orally active muscle relaxant and is used in treating the spasticity and muscle rigidity of spinal cord injuries, cereb ...
4.7.4.2 GABA Antagonists An important direct antagonist is the alkaloid (+)-bicuculline (4.175), which binds to all synaptic GAB ...
provide leads in drug discovery. Quantum pharmacology calculations have been used to designin silicolibraries of benzodiazepine ...
cardiac patients. These previous analogs are termed 1,4-benzodiazepines since the two nitrogen atoms within the diazepine ring a ...
of compounds with affinity for these receptors are not benzodiazepines, it may be more acceptable to employ the alternative nome ...
the slow entry of the resultant molecule into the CNS affects the onset of action. Aromatic substituents produce anticonvulsant ...
4.7.7 GABAergic Drugs: Anticonvulsants Benzodiazepines and barbiturates are used as anticonvulsant drugs in the treatment of epi ...
doses; at high doses, it also inhibits succinic semialdehyde dehydrogenase, the enzyme oxidizing the semialdehyde. As this metab ...
4.7.9 The Clinical–Molecular Interface: Huntington’s Disease as a GABAergic Disorder Huntington’s disease or Huntington’s chorea ...
terminated by cellular re-uptake, mediated through a high-affinity transporter system. There are two glycine receptors: the stry ...
This compound has displayed significant activity in animal models of epilepsy (maximal electroshock assay) and stroke (focal isc ...
4.9.1 Glutamate Receptors The array of receptors that mediate the activities of glutamate is somewhat confusing. Broadly speakin ...
agonist. Likewise, with appropriate substitutions and replacement, glutamic acid analogs can also be competitive antagonists. In ...
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