Potential probe for examining opiate-receptor interactions: model compound study of dynamic effects on /sup 15/N INEPT enhancements

Journal Article · Thu Oct 01 00:00:00 EDT 1987 · J. Pharm. Sci.; (United States)

DOI:https://doi.org/10.1002/jps.2600761013· OSTI ID:5303280

Schilling, K H; Mikita, M A

Model systems were chosen in an attempt to mimic the proton exchange environment of an agonist nitrogen in an opiate-receptor interaction. The two model systems studied were an ammonium: 18-crown-6 ether complex and a quinuclidine-trifluoroacetic acid ion pair. Each system was examined for their effects on /sup 15/N NMR INEPT enhancements. Both models were found to retard proton exchange dynamics, as observed by increased enhancements relative to free ions in neutral aqueous solutions. These results suggest that the confinement of a protonated nitrogen, such as that expected in receptor binding, may alter exchange dynamics to favor INEPT enhancements, while unbound agonists would remain unenhanced. As a result, /sup 15/N NMR INEPT enhancements from a solution of receptor subtypes with an appropriate /sup 15/N-labeled agonist may present a means of exploring the dynamics of direct opiate-receptor interactions.

• Research Organization: Univ. of Colorado, Denver (USA)
• OSTI ID: 5303280
• Journal Information: J. Pharm. Sci.; (United States), Vol. 76:10
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
ENDORPHINS
RECEPTORS
ION EXCHANGE
AQUEOUS SOLUTIONS
BIOLOGICAL MODELS
NITROGEN 15
NUCLEAR MAGNETIC RESONANCE
PROTONS
AUTONOMIC NERVOUS SYSTEM AGENTS
BARYONS
DISPERSIONS
DRUGS
ELEMENTARY PARTICLES
FERMIONS
HADRONS
ISOTOPES
LIGHT NUCLEI
MAGNETIC RESONANCE
MEMBRANE PROTEINS
MIXTURES
NEUROREGULATORS
NITROGEN ISOTOPES
NUCLEI
NUCLEONS
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
PROTEINS
RESONANCE
SOLUTIONS
STABLE ISOTOPES
550201* - Biochemistry- Tracer Techniques