Structural derivatives of pindolol: relationship between in vivo and in vitro potencies for their interaction with central beta-adrenergic receptors

Journal Article · Mon Aug 24 00:00:00 EDT 1987 · Life Sci.; (United States)

DOI:https://doi.org/10.1016/0024-3205(87)90688-6· OSTI ID:6075734

Tejani-Butt, S M; Brunswick, D J

Although (-)-/sup 125/I-iodopindolol (IPIN) can be used to label beta-adrenergic receptors in the central nervous system (CNS) in vivo, use of this ligand for receptor imaging studies in humans may be limited due to its relatively poor penetration into the CNS. A series of derivatives related to pindolol was therefore studied in an effort to determine the factors that might influence the penetration and interaction of these compounds with central beta-adrenergic receptors in vivo. Evaluation of the ability of these derivatives to displace the binding of IPIN in the brain upon systemic administration provides an assessment of whether the derivatives penetrate and interact with central beta-adrenergic receptors in vivo. Multiple regression analyses showed that the most important factor which influences the ability of the pindolol derivatives to penetrate into the brain and interact with beta-adrenergic receptors in vivo is the affinity of the derivatives for binding to beta-adrenergic receptors in vitro. Both lipophilicity and the molecular weights of the derivatives are important secondary factors which influence their in vivo potency. 15 references, 4 figures, 1 table.

• Research Organization: Univ. of Pennsylvania School of Medicine and Neuropsychopharmacology Unit, Philadelphia
• OSTI ID: 6075734
• Journal Information: Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 41:8; ISSN LIFSA
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
ALCOHOLS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
CENTRAL NERVOUS SYSTEM
DATA
DAYS LIVING RADIOISOTOPES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
EXPERIMENTAL DATA
HYDROXY COMPOUNDS
IN VITRO
IN VIVO
INFORMATION
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
MATHEMATICS
MEMBRANE PROTEINS
MOLECULAR WEIGHT
NERVOUS SYSTEM
NUCLEI
NUMERICAL DATA
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
PROPANOLS
PROTEINS
RADIOISOTOPES
REACTION KINETICS
RECEPTORS
REGRESSION ANALYSIS
STATISTICS
SYMPATHOMIMETICS
TRACER TECHNIQUES