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Titolo:
(Extra)thermodynamics of the drug-receptor interaction
Autore:
Raffa, RB;
Indirizzi:
Temple Univ, Sch Pharm, Dept Pharmaceut Sci, Philadelphia, PA 19140 USA Temple Univ Philadelphia PA USA 19140 eut Sci, Philadelphia, PA 19140 USA Temple Univ, Sch Med, Dept Pharmacol, Philadelphia, PA 19140 USA Temple Univ Philadelphia PA USA 19140 armacol, Philadelphia, PA 19140 USA
Titolo Testata:
LIFE SCIENCES
fascicolo: 10, volume: 65, anno: 1999,
pagine: 967 - 980
SICI:
0024-3205(19990730)65:10<967:(OTDI>2.0.ZU;2-N
Fonte:
ISI
Lingua:
ENG
Soggetto:
ENTHALPY-ENTROPY COMPENSATION; OPIOID-DELTA RECEPTORS; THERMODYNAMIC ANALYSIS; VANT HOFF; BINDING;
Keywords:
thermodynamics; enthalpy; entropy; free energy; drug-receptor interaction;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
29
Recensione:
Indirizzi per estratti:
Indirizzo: Raffa, RB Temple Univ, Sch Pharm, Dept Pharmaceut Sci, 3307 N Broad St, Philadelphia, PA 19140 USA Temple Univ 3307 N Broad St Philadelphia PA USA 19140 19140 USA
Citazione:
R.B. Raffa, "(Extra)thermodynamics of the drug-receptor interaction", LIFE SCI, 65(10), 1999, pp. 967-980

Abstract

A core concept in pharmacology is drug-receptor affinity, i.e., the tendency of a drug molecule to bind to one or more receptors due to the collective influence of multiple molecular forces. The estimation of affinity as a dissociation constant (reciprocal of the equilibrium constant) is extraordinarily valuable. However, elucidation of the nature of the underlying concept-i.e., what accounts for affinity-is not achievable using such a static measure. Observing how the system responds to a perturbation (e.g., to a change in temperature) reveals more fundamental information. The present reviewsummarizes the general concepts of thermodynamic analysis applied to drug-receptor interactions and discusses 'extrathermodynamic' phenomena, such asenthalpy-entropy 'compensation'. Together, these concepts may provide insight into the: nature of drug-receptor interactions, begin to elucidate the forces that underlie such interactions-and begin to define and refine more nebulous terms such as affinity.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 29/05/20 alle ore 17:02:31