/sup 13/C NMR studies of the molecular flexibility of antidepressants
Journal Article
·
· J. Pharm. Sci.; (United States)
The solution dynamics of a series of clinically potent antidepressants have been investigated by measuring /sup 13/C NMR relaxation parameters. Correlation times and internal motional rates were calculated from spin-lattice relaxation times and nuclear Overhauser effects for the protonated carbons in mianserin, imipramine-like antidepressants, and amitriptyline-like antidepressants. These data were interpreted in terms of overall molecular tumbling, internal rotations, and inherent flexibility of these structures. Of particular interest was the conformational variability of the tricyclic nucleus of the tricyclic antidepressants, where the data indicated a fivefold difference in mobility of the dimethylene bridge of imipramine-like antidepressants relative to amitriptyline-like compounds. The implications of such a difference in internal motions is discussed in relation to previous NMR studies and to the reported differences in pharmacological activity of these antidepressants.
- Research Organization:
- Victorian College of Pharmacy, Ltd., Parkville, Australia
- OSTI ID:
- 5811221
- Journal Information:
- J. Pharm. Sci.; (United States), Journal Name: J. Pharm. Sci.; (United States) Vol. 2; ISSN JPMSA
- Country of Publication:
- United States
- Language:
- English
Similar Records
Inhibition of /sup 22/Na influx by tricyclic and tetracyclic antidepressants and binding of (/sup 3/H)imipramine in bovine adrenal medullary cells
Effects of antidepressant drugs on histamine-H/sub 1/ receptors in the brain
Differential binding of /sup 3/H-imipramine and /sup 3/H-mianserin in rat cerebral cortex
Journal Article
·
Thu Oct 01 00:00:00 EDT 1987
· J. Pharmacol. Exp. Ther.; (United States)
·
OSTI ID:5786239
Effects of antidepressant drugs on histamine-H/sub 1/ receptors in the brain
Journal Article
·
Sun Feb 05 23:00:00 EST 1984
· Life Sci.; (United States)
·
OSTI ID:6304590
Differential binding of /sup 3/H-imipramine and /sup 3/H-mianserin in rat cerebral cortex
Journal Article
·
Sun Nov 15 23:00:00 EST 1981
· Life Sci.; (United States)
·
OSTI ID:5801965
Related Subjects
550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ANTIDEPRESSANTS
CARBON 13
CARBON ISOTOPES
CENTRAL NERVOUS SYSTEM AGENTS
DRUGS
EVEN-ODD NUCLEI
FLEXIBILITY
HYDROGEN COMPOUNDS
ISOTOPE APPLICATIONS
ISOTOPES
LIGHT NUCLEI
MAGNETIC RESONANCE
MECHANICAL PROPERTIES
MOLECULAR STRUCTURE
NUCLEAR MAGNETIC RESONANCE
NUCLEI
OVERHAUSER EFFECT
OXYGEN COMPOUNDS
PSYCHOTROPIC DRUGS
RELAXATION
RESONANCE
SOLVENTS
SPIN-LATTICE RELAXATION
STABLE ISOTOPES
TENSILE PROPERTIES
TRACER TECHNIQUES
WATER
59 BASIC BIOLOGICAL SCIENCES
ANTIDEPRESSANTS
CARBON 13
CARBON ISOTOPES
CENTRAL NERVOUS SYSTEM AGENTS
DRUGS
EVEN-ODD NUCLEI
FLEXIBILITY
HYDROGEN COMPOUNDS
ISOTOPE APPLICATIONS
ISOTOPES
LIGHT NUCLEI
MAGNETIC RESONANCE
MECHANICAL PROPERTIES
MOLECULAR STRUCTURE
NUCLEAR MAGNETIC RESONANCE
NUCLEI
OVERHAUSER EFFECT
OXYGEN COMPOUNDS
PSYCHOTROPIC DRUGS
RELAXATION
RESONANCE
SOLVENTS
SPIN-LATTICE RELAXATION
STABLE ISOTOPES
TENSILE PROPERTIES
TRACER TECHNIQUES
WATER