BIOMAT Database Logo BIOMAT Database Logo

Non-adrenoceptor [3H]idazoxan binding sites (I2-imidazoline sites) are increased in postmortem brain from patients with Alzheimer's disease. 1993

J Ruiz, and I Martín, and L F Callado, and J J Meana, and F Barturen, and J A García-Sevilla
Department of Pharmacology, University of the Basque Country, Leioa, Spain.

The I2-imidazoline site (a non-adrenergic mitochondrial site for which a glial location has been proposed and that is associated with the B-form of the enzyme monoamine oxidase) was evaluated in postmortem cortical membranes from 9 subjects with Alzheimer's disease (AD) and 9 matched-controls by using [3H]idazoxan (0.6-30 nM) in the presence of 10(-6) M (-)-adrenaline to prevent binding to alpha 2-adrenoceptors. In AD the density (Bmax) of I2-imidazoline sites was significantly higher (+63%) than in controls whereas no differences were apparent in affinity values (Kd). The results support the hypothesis that the I2 imidazoline site has a major location on glial (astrocyte) cells.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D008566 Membranes Thin layers of tissue which cover parts of the body, separate adjacent cavities, or connect adjacent structures. Membrane Tissue,Membrane,Membrane Tissues,Tissue, Membrane,Tissues, Membrane
D011955 Receptors, Drug Proteins that bind specific drugs with high affinity and trigger intracellular changes influencing the behavior of cells. Drug receptors are generally thought to be receptors for some endogenous substance not otherwise specified. Drug Receptors,Drug Receptor,Receptor, Drug
D004146 Dioxanes Compounds that contain the structure 1,4-dioxane.
D004837 Epinephrine The active sympathomimetic hormone from the ADRENAL MEDULLA. It stimulates both the alpha- and beta- adrenergic systems, causes systemic VASOCONSTRICTION and gastrointestinal relaxation, stimulates the HEART, and dilates BRONCHI and cerebral vessels. It is used in ASTHMA and CARDIAC FAILURE and to delay absorption of local ANESTHETICS. Adrenaline,4-(1-Hydroxy-2-(methylamino)ethyl)-1,2-benzenediol,Adrenaline Acid Tartrate,Adrenaline Bitartrate,Adrenaline Hydrochloride,Epifrin,Epinephrine Acetate,Epinephrine Bitartrate,Epinephrine Hydrochloride,Epinephrine Hydrogen Tartrate,Epitrate,Lyophrin,Medihaler-Epi,Acetate, Epinephrine
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000317 Adrenergic alpha-Antagonists Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma. Adrenergic alpha-Receptor Blockaders,alpha-Adrenergic Blocking Agents,alpha-Adrenergic Receptor Blockaders,alpha-Blockers, Adrenergic,Adrenergic alpha-Blockers,alpha-Adrenergic Antagonists,alpha-Adrenergic Blockers,Adrenergic alpha Antagonists,Adrenergic alpha Blockers,Adrenergic alpha Receptor Blockaders,Agents, alpha-Adrenergic Blocking,Antagonists, alpha-Adrenergic,Blockaders, Adrenergic alpha-Receptor,Blockaders, alpha-Adrenergic Receptor,Blockers, alpha-Adrenergic,Blocking Agents, alpha-Adrenergic,Receptor Blockaders, alpha-Adrenergic,alpha Adrenergic Antagonists,alpha Adrenergic Blockers,alpha Adrenergic Blocking Agents,alpha Adrenergic Receptor Blockaders,alpha Blockers, Adrenergic,alpha-Antagonists, Adrenergic,alpha-Receptor Blockaders, Adrenergic
D000368 Aged A person 65 years of age or older. For a person older than 79 years, AGED, 80 AND OVER is available. Elderly

Related Publications

J Ruiz, and I Martín, and L F Callado, and J J Meana, and F Barturen, and J A García-Sevilla
Presynaptic imidazoline receptors and non-adrenoceptor [3H]-idazoxan binding sites in human cardiovascular tissues.
September 1997, British journal of pharmacology,
J Ruiz, and I Martín, and L F Callado, and J J Meana, and F Barturen, and J A García-Sevilla
Pharmacological modulation of immunoreactive imidazoline receptor proteins in rat brain: relationship with non-adrenoceptor [3H]-idazoxan binding sites.
August 1996, British journal of pharmacology,
J Ruiz, and I Martín, and L F Callado, and J J Meana, and F Barturen, and J A García-Sevilla
I2-imidazoline binding sites and monoamine oxidase activity in human postmortem brain from patients with Parkinson's disease.
January 1997, Neurochemistry international,
J Ruiz, and I Martín, and L F Callado, and J J Meana, and F Barturen, and J A García-Sevilla
[3H]idazoxan binds to mitochondrial I2 imidazoline binding sites in isolated cells from rabbit kidney proximal tubule.
July 1995, Annals of the New York Academy of Sciences,
J Ruiz, and I Martín, and L F Callado, and J J Meana, and F Barturen, and J A García-Sevilla
[3H]idazoxan binding to bovine adrenal medullary membranes: identification and pharmacological characterization of I2-imidazoline sites.
September 1994, Naunyn-Schmiedeberg's archives of pharmacology,
J Ruiz, and I Martín, and L F Callado, and J J Meana, and F Barturen, and J A García-Sevilla
Imidazoline (I2) binding sites in chicken brain.
June 1999, Annals of the New York Academy of Sciences,
J Ruiz, and I Martín, and L F Callado, and J J Meana, and F Barturen, and J A García-Sevilla
Opposite age-dependent changes of alpha 2A-adrenoceptors and nonadrenoceptor [3H]idazoxan binding sites (I2-imidazoline sites) in the human brain: strong correlation of I2 with monoamine oxidase-B sites.
September 1993, Journal of neurochemistry,
J Ruiz, and I Martín, and L F Callado, and J J Meana, and F Barturen, and J A García-Sevilla
Species-selective binding of [3H]-idazoxan to alpha 2-adrenoceptors and non-adrenoceptor, imidazoline binding sites in the central nervous system.
July 1993, British journal of pharmacology,
J Ruiz, and I Martín, and L F Callado, and J J Meana, and F Barturen, and J A García-Sevilla
Pentamidine is a potent inhibitor of [3H]idazoxan binding to imidazoline I2 receptors.
June 1999, Annals of the New York Academy of Sciences,
J Ruiz, and I Martín, and L F Callado, and J J Meana, and F Barturen, and J A García-Sevilla
1,5-Bis(4-amidinophenoxy)pentane (pentamidine) is a potent inhibitor of [3H]idazoxan binding to imidazoline I2 binding sites.
July 1998, European journal of pharmacology,
Copied contents to your clipboard!