Effect of alpha-methyldopa on alpha-noradrenergic receptor binding sites in the mouse brain. 1984

M Oide

alpha-Methyldopa (alpha-MD) was administered intraperitoneally into adult male mice and its effect on alpha 1- and alpha 2-noradrenergic receptor binding sites in the brain was investigated, using [3H]WB-4101 and [3H]clonidine, respectively. A single injection of 50-200 mg/kg alpha-MD abolished the high affinity binding to alpha 2-receptor sites and only the low affinity binding was observed with lower Bmax values. A significant effect of alpha-MD on alpha 1-receptor sites was not detected even after repeated injections (200 mg/kg/day X 3). Pretreatment with fusaric acid or diethyldithiocarbamate (inhibitors of dopamine-beta-hydroxylase) exerted no influence on the actions of alpha-MD on alpha 2-receptor sites, whereas NSD-1055 (an inhibitor of dopa decarboxylase) inhibited the effects of alpha-MD. It is concluded, therefore, that alpha-methyldopamine, a decarboxylated metabolite of alpha-MD, may be responsible for the reducing effect of alpha-MD on alpha 2-receptor sites.

UI MeSH Term Description Entries
D008297 Male Males
D008750 Methyldopa An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent. Methyldopate,alpha-Methyldopa,Aldomet,Alphamethyldopa,Apo-Methyldopa,Dopamet,Dopegit,Dopegyt,Dopergit,Hydopa,Meldopa,Nu-Medopa,Sembrina,alpha-Methyl-L-Dopa,Apo Methyldopa,Nu Medopa,alpha Methyl L Dopa,alpha Methyldopa
D008781 Methyltyrosines A group of compounds that are methyl derivatives of the amino acid TYROSINE.
D008815 Mice, Inbred Strains Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations, or by parent x offspring matings carried out with certain restrictions. All animals within an inbred strain trace back to a common ancestor in the twentieth generation. Inbred Mouse Strains,Inbred Strain of Mice,Inbred Strain of Mouse,Inbred Strains of Mice,Mouse, Inbred Strain,Inbred Mouse Strain,Mouse Inbred Strain,Mouse Inbred Strains,Mouse Strain, Inbred,Mouse Strains, Inbred,Strain, Inbred Mouse,Strains, Inbred Mouse
D011941 Receptors, Adrenergic Cell-surface proteins that bind epinephrine and/or norepinephrine with high affinity and trigger intracellular changes. The two major classes of adrenergic receptors, alpha and beta, were originally discriminated based on their cellular actions but now are distinguished by their relative affinity for characteristic synthetic ligands. Adrenergic receptors may also be classified according to the subtypes of G-proteins with which they bind; this scheme does not respect the alpha-beta distinction. Adrenergic Receptors,Adrenoceptor,Adrenoceptors,Norepinephrine Receptor,Receptors, Epinephrine,Receptors, Norepinephrine,Adrenergic Receptor,Epinephrine Receptors,Norepinephrine Receptors,Receptor, Adrenergic,Receptor, Norepinephrine
D011942 Receptors, Adrenergic, alpha One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation. Adrenergic alpha-Receptor,Adrenergic alpha-Receptors,Receptors, alpha-Adrenergic,alpha-Adrenergic Receptor,alpha-Adrenergic Receptors,Receptor, Adrenergic, alpha,Adrenergic alpha Receptor,Adrenergic alpha Receptors,Receptor, alpha-Adrenergic,Receptors, alpha Adrenergic,alpha Adrenergic Receptor,alpha Adrenergic Receptors,alpha-Receptor, Adrenergic,alpha-Receptors, Adrenergic
D012110 Reserpine An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use. Raunervil,Raupasil,Rausedil,Rausedyl,Serpasil,Serpivite,V-Serp,V Serp
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D001958 Brocresine A histidine decarboxylase inhibitor. NSD-1055,NSD 1055,NSD1055
D003000 Clonidine An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION. Catapres,Catapresan,Catapressan,Chlophazolin,Clofelin,Clofenil,Clonidine Dihydrochloride,Clonidine Hydrochloride,Clonidine Monohydrobromide,Clonidine Monohydrochloride,Clopheline,Dixarit,Gemiton,Hemiton,Isoglaucon,Klofelin,Klofenil,M-5041T,ST-155,Dihydrochloride, Clonidine,Hydrochloride, Clonidine,M 5041T,M5041T,Monohydrobromide, Clonidine,Monohydrochloride, Clonidine,ST 155,ST155
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