Clonidine binds to imidazole binding sites as well as alpha 2-adrenoceptors in the ventrolateral medulla

European Journal of Pharmacology
P ErnsbergerD J Reis

Abstract

Binding sites labeled by [3H]p-aminoclonidine ([3H]PAC) were characterized in bovine brain membranes prepared from the ventrolateral medulla, the probable site of the antihypertensive action of clonidine and analogs. Comparison was made with [3H]PAC binding to membranes prepared from frontal cortex, which has been studied extensively. Saturation binding isotherms for [3H]PAC were similar in the two regions, although Bmax values were approximately two-fold lower in ventrolateral medulla relative to frontal cortex. Norepinephrine and other phenylethylamines displaced [3H]PAC from a maximum of 70% of the total sites in the ventrolateral medulla. The remaining 30% were norepinephrine-insensitive, non-adrenoceptor sites which displayed high affinity for imidazole compounds. Ligand selectivity differed markedly between ventrolateral medulla and frontal cortex, since some imidazole compounds which potently inhibited [3H]PAC binding in the ventrolateral medulla had no effect in frontal cortex. Imidazole binding sites may mediate, in part, the hypotensive action of clonidine and other imidazole compounds in the ventrolateral medulla. These sites may also participate in the functions of a putative endogenous clonidine-like substance.

References

Jun 1, 1977·The Journal of Pharmacy and Pharmacology·R R RuffoloP N Patil
Jan 1, 1978·Reviews of Physiology, Biochemistry and Pharmacology· Kobinger
Aug 15, 1978·European Journal of Pharmacology·W P Burkard
Jan 1, 1985·Journal of Cardiovascular Pharmacology·D J Reis
Dec 22, 1985·The Journal of Comparative Neurology·C A RossD J Reis
May 13, 1986·European Journal of Pharmacology·P BousquetD Atlas
Oct 15, 1984·European Journal of Biochemistry·D Atlas, Y Burstein
Sep 1, 1980·Analytical Biochemistry·P J Munson, D Rodbard
Jul 1, 1980·Journal of Neurochemistry·S H Snyder, R R Goodman
Aug 1, 1983·Computer Programs in Biomedicine·G A McPherson
Jan 29, 1981·European Journal of Pharmacology·P BousquetJ Schwartz
Apr 21, 1980·Life Sciences·D A KendallS J Enna
Jul 21, 1980·Life Sciences·T J RisingT P Wood

❮ Previous
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Citations

Feb 1, 1996·Journal of Clinical Pharmacology·A Yu, W H Frishman
Apr 15, 1993·Journal of Neuroscience Research·S RegunathanD J Reis
Dec 1, 1996·Naunyn-Schmiedeberg's Archives of Pharmacology·H IshikawaP N Patil
Dec 1, 1993·Naunyn-Schmiedeberg's Archives of Pharmacology·B SzaboK Starke
Dec 1, 1993·Naunyn-Schmiedeberg's Archives of Pharmacology·M BarriosJ M Baeyens
Jul 1, 1993·Naunyn-Schmiedeberg's Archives of Pharmacology·G J MolderingsM Göthert
Jan 1, 1989·Psychopharmacology·F FerrariV Mangiafico
Jun 1, 1992·Cellular and Molecular Neurobiology·M Ohara-Imaizumi, K Kumakura
Dec 1, 1989·Naunyn-Schmiedeberg's Archives of Pharmacology·A Schulz, A Hasselblatt
Mar 1, 1994·Cardiovascular Drugs and Therapy·P ErnsbergerM O Christen
May 1, 1997·Canadian Journal of Anaesthesia = Journal Canadien D'anesthésie·T KamibayashiM Maze
Jul 24, 2010·Current Psychiatry Reports·L Cinnamon BidwellScott H Kollins
Dec 22, 1994·The American Journal of Cardiology·F Sannajust, G A Head
May 7, 1987·European Journal of Pharmacology·M DontenwillP Bousquet
Sep 13, 1988·European Journal of Pharmacology·F YablonskyJ P Dausse
Feb 9, 1988·European Journal of Pharmacology·C A HamiltonM A Yakubu
May 10, 1988·European Journal of Pharmacology·M DontenwillA Belcourt
Mar 14, 1989·European Journal of Pharmacology·G BriccaP Bousquet
Jan 10, 1989·European Journal of Pharmacology·D Langin, M Lafontan
Dec 12, 1989·European Journal of Pharmacology·P ErnsbergerD J Reis
Feb 13, 1990·European Journal of Pharmacology·M A YakubuJ L Reid
Mar 26, 1991·European Journal of Pharmacology·R E GomezD J Reis
Mar 26, 1991·European Journal of Pharmacology·J W DownieJ B Gajewski
Aug 25, 1992·European Journal of Pharmacology·F TessonA Parini
Nov 30, 1993·European Journal of Pharmacology·F Ferrari, D Giuliani
Feb 23, 1993·European Journal of Pharmacology·A C MacKinnonC M Brown
Nov 14, 1994·European Journal of Pharmacology·H GreneyP Bousquet
May 24, 1995·European Journal of Pharmacology·M Le RouzicS Z Langer

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