Biomaterial Database

Thermodynamics of ligand binding to the cloned delta-opioid receptor. 1996

P A Maguire, and G H Loew

Molecular Research Institute, Palo Alto, CA 94304, USA.

The goal of this study was to determine the relative contribution of entropy and enthalpy to the free energies of binding to recombinant mouse delta-opioid receptors for the peptide agonist, DPDPE ([D-Pen2,D-Pen5]enkephalin), the peptide antagonist, TIPP(psi) (Tyr-Tic(psi)[CH2NH]Phe-Phe-OH), the nonpeptide agonist, SNC80 ((+)-4-[(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl )-3-methoxybenzyl]-N,N-diethylbenzamide), and the nonpeptide antagonist, naltrindole. Competitive binding studies were carried out using [3H]naltrindole at 0 degrees C, 12 degrees C, 25 degrees C and 37 degrees C, the affinities calculated and van't Hoff plots constructed for each ligand. The temperature dependence of binding and van't Hoff plots indicated that the entropy contribution is the major component of the free energy, for all four ligands, independent of its activity or chemical nature.

UI	MeSH Term	Description	Entries
D009842	Oligopeptides	Peptides composed of between two and twelve amino acids.	Oligopeptide
D010879	Piperazines	Compounds that are derived from PIPERAZINE.
D011994	Recombinant Proteins	Proteins prepared by recombinant DNA technology.	Biosynthetic Protein,Biosynthetic Proteins,DNA Recombinant Proteins,Recombinant Protein,Proteins, Biosynthetic,Proteins, Recombinant DNA,DNA Proteins, Recombinant,Protein, Biosynthetic,Protein, Recombinant,Proteins, DNA Recombinant,Proteins, Recombinant,Recombinant DNA Proteins,Recombinant Proteins, DNA
D004745	Enkephalins	One of the three major families of endogenous opioid peptides. The enkephalins are pentapeptides that are widespread in the central and peripheral nervous systems and in the adrenal medulla.	Enkephalin
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D001549	Benzamides	BENZOIC ACID amides.
D013816	Thermodynamics	A rigorously mathematical analysis of energy relationships (heat, work, temperature, and equilibrium). It describes systems whose states are determined by thermal parameters, such as temperature, in addition to mechanical and electromagnetic parameters. (From Hawley's Condensed Chemical Dictionary, 12th ed)	Thermodynamic
D017465	Receptors, Opioid, delta	A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.	Opioid Receptors, delta,Receptors, delta,Receptors, delta Opioid,delta Receptors,delta Opioid Receptor,delta Receptor,Opioid Receptor, delta,Receptor, delta,Receptor, delta Opioid,delta Opioid Receptors
D051379	Mice	The common name for the genus Mus.	Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus
D020881	Enkephalin, D-Penicillamine (2,5)-	A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.	D-Pen2, D-Pen5-Enkephalin,D-Penicillamine (2,5)-Enkephalin,DPDPE,Bis-Pen-Enkephalin,Bis-Penicillamine-Enkephalin,D-Pen2, L-Pen5-Enkephalin,DPDPE(SH)2,DPLPE,Enkephalin, Pen(2,5)-,Enkephalin, Penicillamine (2,5)-,Bis Pen Enkephalin,Bis Penicillamine Enkephalin,D Pen2, D Pen5 Enkephalin,D Pen2, L Pen5 Enkephalin,D-Pen5-Enkephalin D-Pen2,L-Pen5-Enkephalin D-Pen2