- Docente: Carlo Melchiorre
- Credits: 8
- SSD: CHIM/08
- Language: Italian
- Teaching Mode: Traditional lectures
- Campus: Bologna
- Corso: Long cycle 2nd degree programme in Chemistry and Pharmaceutical Technologies (cod. 0038)
Course contents
Neurotransmitter receptors
The bonding of ligands to receptors. Structure and classification of receptors. General mode of operation. Ligand-response relationships: agonist and antagonist concentration-response relationships, partial agonism, inverse agonism. Ligand-receptor theories: Clark's occupancy theory, the rate theory, two-state model, perturbation theory. Classification, localization, function, structure, active site of adrenergic receptors, cholinergic receptors, dopaminergic receptors, GABAergic receptors, and opioid receptors.
Neurotransmitters
Acetylcholine, catecholamines, histamine, 4-aminobutyric acid, enkephalines: biosynthesis, release, uptake, metabolism, molecular properties, active conformation, stereochemical properties.
Drugs acting at neurotransmitter receptors
Structure-activity relationships, mechanism and site of action, therapeutic use, side effects, stereochemistry, and synthetic aspects of drugs acting at adrenergic, dopaminergic, cholinergic, histaminergic, GABAergic, and opioid systems. Stereochemistry and synthesis of selected drugs.
Drug design
Basic principles of rational drug design. Drug design
strategies. Modification of a lead compound.
Readings/Bibliography
C. Melchiorre - I recettori dei neurotrasmettitori: un'introduzione per la chimica farmaceutica - CLUEB, Bologna, 1996.
C. Melchiorre, A. Minarini, M. Recanatini, V. Tumiatti, M.L. Bolognesi - I recettori colinergici - CLUEB, Bologna, 1997.
F. Gualtieri, M.N. Romanelli, E. Teodori - Chimica farmaceutica dei recettori: disegno e sintesi di farmaci e mezzi di indagine farmacologica - CLUEB, Bologna, 1997.
M. Giannella, W. Quaglia - I recettori adrenergici - CLUEB, Bologna, 1998.
G. Ronsisvalle, M. Pappalardo, L. Pasquinucci, O. Prezzavento – I recettori oppioidi – CLUEB, Bologna, 1999.
D. Lednicer, L. A. Mitscher - The organic chemistry of drug synthesis, Voll. 1-6 - John Wiley & Sons, New York, 1977, 1980, 1984, 1990, 1995, 1999.
Office hours
See the website of Carlo Melchiorre