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Docente
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BATTAGLIA GIUSEPPE
(programma)
Receptors: Classification, structural, molecular and functional organization, pharmacological modulation. Regulation of receptor function: desensitisation, up
regulation, down regulation.
Ionotropic receptors: Tissue and subcellular distribution. Molecular organization. Ionic selectivity. Pharmacological modulation.
Scienze Matematiche Fisiche e Naturali - Farmacia pag. 23
Documento generato da GOMP2012 (smart_edu) - www.besmart.it
Metabotropic receptors: Classification. Molecular organization. Ligand binding sites. Mechanisms of interaction with G proteins. Molecular organization and
function of heteromeric G proteins. Effector mechanisms: adenylate cyclase and cAMP, phospholipase C and phosphinositides cycle, MAP kinase cascade.
Scaffolding proteins: localization and functions.
Methods for the study of membrane receptors: Receptor binding studies on membranes and tissues (receptor autoradiography). Methods for the analysis of
G protein coupling to receptors. Principles of immunohistochemistry and electrophysiology.
Protein kinases and their role in signal transduction: Molecular structure and mechanism of action of protein kinases A, C, calcium/calmodulin-dependent,
MAPK. GSK: G protein coupled receptor kinases. Pharmacological modulation of protein kinases. Protein phosphatases. Calcinueurin and
immunosuppressant drugs. Role of phosphorylation in the modulation of receptor function. Regulation of intracellular calcium homeostasis: Structure and
function of calcium channels, pumps and transporters localized on the cell membrane. Voltage-dependent calcium-channels: classification, molecular
organization, voltage sensor, ionic selectivity, pharmacological modulation. Na+/K+-ATPase, Na+/Ca2+ exchanger and cardioactive glycosides. Intracellular
calcium store, ryanodine and IP3 receptors, endogenous and pharmacological modulators. Cytosolic proteins implicated in calcium binding.
Sodium channels: Voltage-dependent sodium channels: molecular organization, functions, voltage sensor, opening and inactivating mechanisms, cellular
localization: cytoskeleton anchoring sites, modulation by drugs and toxins. Epithelial sodium channels: molecular organization and modulation by potassium
spare diuretics.
Potassium channels: Molecular and functional classification. Voltage-gated channels, ATP-dependent channels, GIRKS, inward rectifiers, calcium-activated
channels. Pharmacological modulation of potassium channels.
Chloride channels: Molecular organization and function of CIC and CFTR channels.
Neurotransporters: Molecular structure, activation mechanisms and pharmacological modulation of neurotransporters: membrane Na+/K+-dependent
transporter for EAA, membrane Na+/Cl—dependent transporters for GABA and monoamines, vesicular H+-dependent transporters for amino acids and
acetylcholine.
Catecholaminergic transmission: Biosynthesis, vesicular storage, metabolic degradation and reuptake. e adrenergic and dopaminergic receptors: molecular
organization, function, signal transduction mechanisms, pharmacological modulation.
Cholinergic transmission: Biosynthesis, intracellular storage and metabolism of acetylcholine. Cellular localization, function and structural features of choline
acetyl transferase and cholinesterases. Classification, molecular organization and mechanisms of activation of nicotinic and muscarinic receptors.
Serotonergic transmission: Biosynthesis, metabolism and reuptake of serotonin: pharmacological modulation. Classification, function and modulation of
serotonin receptors.
GABAergic transmission: Synthesis, degradation and reuptake of GABA: pharmacological modulation. GABAA, GABAB and GABAC receptors: molecular
organization, mechanisms of receptor activation and modulation.
Excitatory amino acid transmission: Synthesis, vesicular storage and transport of glutamate. Ionotropic and metabotropic receptors for EEA: classification,
molecular organization, mechanisms of activation and pharmacological modulation.
Nitric oxide: Roles, biosynthesis, NOS synthase: isoforms, regulation and pharmacological modulation.
Opioid system: Roles biosynthesis and metabolism of endogenous opioids. Opioid receptors: molecular organization, mechanisms of receptor activation and
pharmacological modulation.
Cannabinoids: Roles, biosynthesis and metabolism of endocannabinoids. Cannabinoid receptors: molecular organization, mechanisms of receptor activation
and pharmacological modulation.
 REFERENCES:
Goodman and Gilman: The pharmacological basis of therapeutics, XI ed. McGraw-Hill
Clementi F., Fumagalli G.: Farmacologia generale e molecolare, III ed. UTET
Hammond, Cellular and Molecular Neurophysiology, III ed. Academic Press
Casarett & Doull's Toxicology: The Basic Science of Poisons, VII ed. McGraw-Hill
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