PMID: 3754610May 5, 1986

Binding profile of a novel cardioselective muscarine receptor antagonist, AF-DX 116, to membranes of peripheral tissues and brain in the rat

Life Sciences
R HammerH Ladinsky

Abstract

The heterogeneity of muscarine receptors was examined in two brain regions (cerebral cortex and cerebellum) and in some parasympathetically innervated peripheral tissues (heart, salivary gland and intraorbital lacrimal gland), by in vitro binding techniques. As a tool, we used a new antimuscarinic compound, AF-DX 116 (see text for structural formula and chemical name). In competition experiments against 3H-N-methylscopolamine (3H-NMS) or 3H-pirenzepine (3H-PZ), AF-DX 116 was found to bind with high affinity to muscarine receptors in the heart and cerebellum (KD's approximately equal to 115 nM), with intermediate affinity to M1 receptors in neuronal tissue (KD = 760 nM) and with low affinity to receptors in exocrine glands (KD's approximately equal to 3200 nM). Its receptor interaction was found to be of the simple, competitive type. Thus, AF-DX 116 shows a novel cardioselective profile. On the basis of the results which demonstrate that the muscarine receptors in the heart and exocrine glands are clearly distinct, it is proposed that these receptors may be subclassified as M2 cardiac type and M2 glandular type muscarine receptors.

Citations

Jan 1, 1991·Archives of Insect Biochemistry and Physiology·E A AbdallahA T Eldefrawi
Jul 1, 1990·Medicinal Research Reviews·C Melchiorre
Oct 1, 1989·Naunyn-Schmiedeberg's Archives of Pharmacology·P WormsK Biziere
Apr 1, 1988·Pflügers Archiv : European journal of physiology·S Tsuji, K Kuba
Apr 1, 1989·Naunyn-Schmiedeberg's Archives of Pharmacology·K J Van Charldorp, P A Van Zwieten
Dec 1, 1990·Digestive Diseases and Sciences·A PfeifferM Herawi
Jan 1, 1993·Psychopharmacology·J P KanR Boigegrain
Dec 1, 1994·Archives of Pharmacal Research·S W LeeJ G Kim
Jul 1, 1994·European Journal of Drug Metabolism and Pharmacokinetics·E CeredaA Sagrada
Nov 6, 1989·Brain Research·J MurugaianH Sapru
Nov 10, 1987·European Journal of Pharmacology·F MartosR Hammer
Sep 13, 1988·European Journal of Pharmacology·L Noronha-BlobW J Kinnier
Oct 26, 1988·European Journal of Pharmacology·S B FreedmanE A Harley
Mar 15, 1988·European Journal of Pharmacology·E MonferiniH Ladinsky
Sep 23, 1988·European Journal of Pharmacology·X M ZhouH Yoshida
Dec 6, 1988·European Journal of Pharmacology·M Eltze, V Figala
Jul 14, 1988·European Journal of Pharmacology·J P DehayeJ Christophe
Jun 22, 1988·European Journal of Pharmacology·L Nilvebrant, B Sparf
May 20, 1988·European Journal of Pharmacology·K J Van CharldorpP A Van Zwieten
Jul 18, 1989·European Journal of Pharmacology·C SchumacherK Biziere
Apr 25, 1989·European Journal of Pharmacology·N R Newberry, M J Gilbert
May 19, 1989·European Journal of Pharmacology·J C Mak, P J Barnes
Aug 11, 1989·European Journal of Pharmacology·M GalvanC Schudt
Jul 3, 1990·European Journal of Pharmacology·A D MichelR L Whiting
Dec 4, 1990·European Journal of Pharmacology·S Chiba, M Tsukada
Mar 13, 1990·European Journal of Pharmacology·M KajimuraN Honda
Jan 3, 1991·European Journal of Pharmacology·H DoodsN Mayer
Apr 24, 1991·European Journal of Pharmacology·R E HowellL Noronha-Blob
Jan 21, 1992·European Journal of Pharmacology·C R Killingsworth, N E Robinson
Sep 21, 1993·European Journal of Pharmacology·H DoodsW Eberlein
Sep 12, 1994·European Journal of Pharmacology·J N PennefatherF J Mitchelson
May 23, 1996·European Journal of Pharmacology·L Zhang
Apr 1, 1989·Experimental Eye Research·P MallorgaM F Sugrue
Jun 1, 1990·Journal of the Neurological Sciences·P VanderheydenG Vauquelin
Jan 1, 1988·Life Sciences·E GiraldoF Sanchez de La Cuesta
Jan 1, 1989·Life Sciences·H F PitschnerA Wellstein
Feb 1, 1989·Neuropharmacology·N R Newberry, G P Connolly
Mar 1, 1991·Neuropharmacology·A Töröcsik, E S Vizi
Mar 1, 1995·Pharmaceutica acta Helvetiae·E MutschlerG Lambrecht
Jan 1, 1988·Progress in Biophysics and Molecular Biology·H C Hartzell
Nov 1, 1988·Immunopharmacology·L G CostaS D Murphy
Jan 1, 1988·Pharmacology & Therapeutics·F J Mitchelson
Apr 1, 1988·Journal of the Autonomic Nervous System·K Sundaram, H Sapru
May 26, 1995·Brain Research. Developmental Brain Research·S M CanduraL G Costa
Nov 1, 1988·Trends in Pharmacological Sciences·P J BarnesJ Maclagan
Jun 1, 1988·Trends in Pharmacological Sciences·C Melchiorre
Jan 1, 1989·Neurochemistry International·P GoldmanW S Messer
Jan 1, 1989·Neurochemistry International·A SzabóK Gulya
Apr 1, 1994·Neurochemistry International·T HashimotoK Kuriyama
Jan 1, 1992·Progress in Neurobiology·M Inoue, M Yoshii
Sep 1, 1995·Hearing Research·K ChenD A Godfrey
Oct 1, 1992·Comparative Biochemistry and Physiology. C, Comparative Pharmacology and Toxicology·Y Iwabuchi, T Masuhara
Sep 1, 1991·Journal of Chemical Neuroanatomy·J M PalaciosP Ramm
Sep 18, 1990·European Journal of Pharmacology·M WaelbroeckJ Christophe
Sep 18, 1990·European Journal of Pharmacology·A P BraunP V Sulakhe
Aug 1, 1994·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·E BarocelliM Impicciatore
Feb 1, 1994·Comparative Biochemistry and Physiology. Pharmacology, Toxicology and Endocrinology·Y IwabuchiT Masuhara
Aug 15, 2000·European Journal of Pharmacology·S DarrochF J Mitchelson
Apr 6, 2001·European Journal of Pharmacology·A LanzafameF J Mitchelson
Jan 1, 1997·Life Sciences·Frederick J EhlertG W Sawyer
May 17, 2000·Pharmaceutica acta Helvetiae·P Angeli
Mar 25, 2000·Bioorganic & Medicinal Chemistry·J MartinM C Lasne
Dec 14, 1999·Anaesthesia·L Karalliedde
Jan 15, 1988·European Journal of Biochemistry·C AndréD A Strosberg
May 1, 1987·Clinical and Experimental Pharmacology & Physiology·F J Mitchelson
May 1, 1990·British Journal of Pharmacology·R MichelettiA Donetti
Nov 1, 1990·British Journal of Pharmacology·S B FreedmanR Baker
Feb 1, 1991·British Journal of Pharmacology·F Brunner, W R Kukovetz
Nov 1, 1994·British Journal of Pharmacology·A SagradaH Ladinsky
Dec 20, 1993·Annals of the New York Academy of Sciences·T Kubo
Aug 2, 2003·Pancreatology : Official Journal of the International Association of Pancreatology (IAP) ... [et Al.]·Elke Niebergall-Roth, Manfred V Singer
Jan 28, 2014·Neurobiology of Learning and Memory·Susan J BartkoTimothy J Bussey
Jan 1, 1990·Journal of Receptor Research·E MonferiniE Giraldo
Oct 17, 2006·The European Journal of Neuroscience·Daniel Bosch, Susanne Schmid
Mar 1, 1989·Biochemical Pharmacology·W S MesserW Hoss
Sep 1, 1989·British Journal of Pharmacology·S Lazareno, F F Roberts
Jan 1, 1989·Journal of Neurochemistry·C Gulat-MarnayJ C Schwartz
Jan 1, 1990·Journal of Receptor Research·A J van ZwamC A van Ginneken
Apr 15, 1999·Japanese Journal of Pharmacology·M TakedaK Taniyama
Jul 23, 2013·European Journal of Pharmacology·Edilson Dantas da Silva JúniorNeide Hyppolito Jurkiewicz
Jan 1, 1986·Scandinavian Journal of Gastroenterology. Supplement·W Londong
Mar 25, 1991·European Journal of Pharmacology·E M WhithamS R Nahorski
Jan 1, 1995·Journal of Psychopharmacology·M SaminiM R Zarrindast
Apr 1, 1989·Pharmacology & Toxicology·P G GillbergC Post
Jul 28, 2005·The Journal of Pharmacology and Experimental Therapeutics·Frederick J Ehlert
Apr 1, 1996·Journal of Cardiovascular Pharmacology·L S SunY Vulliemoz
Jul 1, 1988·Medicinal Research Reviews·W H MoosE R Gamzu
Dec 1, 1987·British Journal of Pharmacology·A D Michel, R L Whiting
Nov 26, 2010·Alternatives to Laboratory Animals : ATLA·Gaurav KaithwasDipak K Majumdar
Feb 1, 1989·British Journal of Pharmacology·R E DelmendoR L Whiting
Mar 1, 1988·British Journal of Pharmacology·E A KunyszR L Whiting
Jan 1, 1989·Naunyn-Schmiedeberg's Archives of Pharmacology·P A LucchesiT W Honeyman
Jul 1, 1989·British Journal of Pharmacology·A D MichelR L Whiting
Mar 16, 2002·Journal of Applied Physiology·William M L BowerfindDavid B Jacoby
Aug 15, 1988·FEBS Letters·J C Henquin, M Nenquin

Related Concepts

AFDX 116
Metazoa
Benzodiazepinones
Plasma Membrane
Cerebellum
Insula of Reil
Lacrimal Gland Structure
Myocardium
Tissue Specificity
Antispasmodic Effect

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