Guanylpirenzepine distinguishes between neuronal ml and m4 muscarinic receptor subtypes

Journal Article · Mon Jan 01 00:00:00 EST 1990 · Journal of Receptor Research; (USA)

DOI:https://doi.org/10.3109/10799899009064659· OSTI ID:5989068

Monferini, E; Cereda, E; Ladinsky, H; Donetti, A; Giraldo, E ^[1]

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1. Istituto De Angeli S.p.A., Milan (Italy)

Guanylpirenzepine, a polar, non-quaternary analog of pirenzepine, exhibited a novel binding behavior in rat brain regions: in competition binding experiments against (3H)pirenzepine labeling the M1 receptor in membranes from cerebral cortex, hippocampus and striatum, the compound, differently from pirenzepine, displayed heterogeneous binding curves. Computer assisted analysis of these curves, evidenced the existence of two populations of binding sites: a large proportion (84-89%) of high affinity receptors (KH = 64-92 nM) and a remainder with very low affinity (KL = 19-28 microM). Like pirenzepine, guanylpirenzepine showed low affinity for the glandular M3 and the cardiac M2 receptors when (3H)N-methylscopolamine was used to label the receptors in membranes from these two tissues; affinity values for guanylpirenzepine were 1336 and 5790 nM respectively, vs 323 and 683 nM for pirenzepine. We conclude that guanylpirenzepine is able to discriminate between m1 and m4 receptor subtypes and may represent a new tool for deeper studies on muscarinic receptors classification.

• OSTI ID: 5989068
• Journal Information: Journal of Receptor Research; (USA), Vol. 10:1-2; ISSN 0197-5110
• Country of Publication: United States
• Language: English

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59 BASIC BIOLOGICAL SCIENCES
ANTIPYRETICS
BIOCHEMICAL REACTION KINETICS
PARASYMPATHOMIMETICS
RECEPTORS
BRAIN
CELL MEMBRANES
COMPUTER CALCULATIONS
CPB
HEART
NERVE CELLS
RATS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ANIMAL CELLS
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BODY
CARDIOVASCULAR SYSTEM
CELL CONSTITUENTS
CENTRAL NERVOUS SYSTEM
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DRUGS
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ISOTOPE APPLICATIONS
KINETICS
MAMMALS
MEMBRANE PROTEINS
MEMBRANES
NERVOUS SYSTEM
ORGANIC COMPOUNDS
ORGANS
PROTEINS
REACTION KINETICS
RODENTS
SOMATIC CELLS
VERTEBRATES
550201* - Biochemistry- Tracer Techniques