Time course of changes in [3H]prazosin binding after catecholaminergic denervation by 6-hydroxydopamine in rat cerebral cortex. Inhibitory effects of ascorbic acid on the alpha 1-adrenoceptor. 1983

C Wolfman, and M Levi de Stein, and E De Robertis

The binding of [3H]prazosin to alpha 1-adrenoceptors was studied in membranes isolated from the rat cerebral cortex, at different times after the intraventricular injection of 6-hydroxydopamine. In controls, the binding was saturable with the Bmax = 113 pmol/g protein and KD = 0.93 nM, and revealed a single class of sites. After the action of the neurotoxin there was an increase in binding that reached +68% after 7 days and +35% after 14 days. This effect corresponded to an increase in Bmax (190 pmol/g protein) and a decrease in affinity (Kd = 2.1 nM), at 7 days after 6-hydroxydopamine. Carrying on experiments without ascorbic acid in the diluent, the well known inhibitory effect in vitro, that this drug has on the binding of several receptor ligands, was confirmed in vivo. The results obtained suggest that the noradrenergic denervation produced by the neurotoxin is capable of inducing adaptive changes, in alpha 1-post-synaptic adrenoceptors as measured by the binding of [3H]prazosin.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D011224 Prazosin A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION. Furazosin,Minipress,Pratsiol,Prazosin HCL,Prazosin Hydrochloride,HCL, Prazosin,Hydrochloride, Prazosin
D011799 Quinazolines A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring. Quinazoline
D011919 Rats, 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. This also includes animals with a long history of closed colony breeding. August Rats,Inbred Rat Strains,Inbred Strain of Rat,Inbred Strain of Rats,Inbred Strains of Rats,Rat, Inbred Strain,August Rat,Inbred Rat Strain,Inbred Strain Rat,Inbred Strain Rats,Inbred Strains Rat,Inbred Strains Rats,Rat Inbred Strain,Rat Inbred Strains,Rat Strain, Inbred,Rat Strains, Inbred,Rat, August,Rat, Inbred Strains,Rats Inbred Strain,Rats Inbred Strains,Rats, August,Rats, Inbred Strain,Strain Rat, Inbred,Strain Rats, Inbred,Strain, Inbred Rat,Strains, Inbred Rat
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
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
D002395 Catecholamines A general class of ortho-dihydroxyphenylalkylamines derived from TYROSINE. Catecholamine,Sympathin,Sympathins
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
D005260 Female Females

Related Publications

C Wolfman, and M Levi de Stein, and E De Robertis
January 1987, Journal of neural transmission,
C Wolfman, and M Levi de Stein, and E De Robertis
August 1986, Fiziologicheskii zhurnal SSSR imeni I. M. Sechenova,
C Wolfman, and M Levi de Stein, and E De Robertis
February 1994, Journal of receptor research,
C Wolfman, and M Levi de Stein, and E De Robertis
February 1982, European journal of pharmacology,
C Wolfman, and M Levi de Stein, and E De Robertis
December 1991, British journal of pharmacology,
C Wolfman, and M Levi de Stein, and E De Robertis
September 1986, Biulleten' eksperimental'noi biologii i meditsiny,
C Wolfman, and M Levi de Stein, and E De Robertis
February 1989, British journal of pharmacology,
Copied contents to your clipboard!