Inhibition of neuronal noradrenaline transport (uptake1) and desipramine binding by amiloride and ethylisopropylamiloride

1989 ◽  
Vol 340 (5) ◽  
Author(s):  
E. Sch�mig ◽  
Jutta Michael-Hepp ◽  
C.L. Sch�nfeld
Keyword(s):  
Desipramine Binding

MOLECULAR MECHANISMS IN IMIPRAMINE AND DESIPRAMINE BINDING TO SYNAPTIC MEMBRANES

1984 ◽  
Vol 7 ◽  
pp. S160 ◽  
Author(s):  
S. Z. Langer ◽  
T. Tateishi ◽  
A. Segonzac ◽  
H. Schoemaker ◽  
C. R. Lee
Keyword(s):  
Molecular Mechanisms ◽  
Synaptic Membranes ◽  
Desipramine Binding

Synthesis of (2-(phenylthio)phenyl)acetamidines and related amidoximes as potential antidepressants

1988 ◽  
Vol 53 (2) ◽  
pp. 381-388 ◽  
Author(s):  
Karel Šindelář ◽  
Zdeněk Šedivý ◽  
Marta Hrubantová ◽  
Martin Valchář ◽  
Jiřina Metyšová ◽  
...  
Keyword(s):  
Binding Sites ◽  
The Other ◽  
Rat Hypothalamus ◽  
Other Hand ◽  
Phenyl Acetonitrile ◽  
Desipramine Binding

Reactions of ethyl(2-(phenylthio)phenyl)acetimidate (X) hydrochloride with ammonia and the corresponding amines resulted in amidines V-X. Heating (2-(phenylthio)phenyl)acetonitrile with 2-aminoethylammonium toluene-4-sulfonate led to the 2-imidazoline XI. Reactions of (2-(phenylthio)phenyl)acetonitrile and the lower homologue with hydroxylamine gave the amidoximes XIII and XV; XIII was oxidized to the sulfoxide XIV. Compounds VII, XI, and XIII showed some antireserpine activity which indicates thymoleptic and antidepressant potentiality. On the other hand, none of the compounds tested did show any noteworthy affinity to the [3H]imipramine and [3H]desipramine binding sites in the rat hypothalamus.

Characterization and ontogenesis of [3H]-desipramine binding sites in developing fetal rat cerebral cells in culture

1980 ◽  
Vol 29 (12) ◽  
pp. 1755-1757 ◽  
Author(s):  
Anat Biegon ◽  
Ziva Yavin ◽  
Ephraim Yavin ◽  
David Samuel
Keyword(s):  
Binding Sites ◽  
Cells In Culture ◽  
Fetal Rat ◽  
Desipramine Binding

Dual Effects of Intravenous Anesthetics on the Function of Norepinephrine Transporters

2000 ◽  
Vol 93 (5) ◽  
pp. 1329-1335 ◽  
Author(s):  
Koji Hara ◽  
Nobuyuki Yanagihara ◽  
Kouichiro Minami ◽  
Hideyasu Hirano ◽  
Takeyoshi Sata ◽  
...  
Keyword(s):  
Term Treatment ◽  
Scatchard Analysis ◽  
Dependent Manner ◽  
Short Term Treatment ◽  
Intravenous Anesthetics ◽  
Norepinephrine Uptake ◽  
Long Term Treatment ◽  
Desipramine Binding ◽  
Neuronal Transmission

Background Norepinephrine transporters (NETs) terminate the neuronal transmission of norepinephrine, which is released from noradrenergic neurons. To investigate the interaction with NET, the authors examined the effects of short- and long-term treatment with anesthetics on the activity and mRNA level of NET. Methods To assay [3H]norepinephrine uptake, bovine adrenal medullary cells in culture were incubated with [3H]norepinephrine in the presence of intravenous anesthetics, including propofol, thiamylal, and diazepam. To study the direct interaction between the anesthetics and NET, the effect of propofol on the binding of [3H]desipramine to the plasma membrane was examined. To study the long-term effect of anesthetics, [3H]norepinephrine uptake by cells pretreated with propofol for 6-24 h and [3H]desipramine binding after pretreatment for 12 h were measured. Simultaneously, we examined the effect of anesthetics on the expression of NET mRNA using the reverse transcriptase-polymerase chain reaction. Results All of the intravenous anesthetics inhibited [3H]norepinephrine uptake in a concentration-dependent manner. The active concentrations of propofol (1-3 microm) and thiamylal (< or = 30 microm) were similar to those encountered clinically. The kinetic analysis revealed that all the anesthetics noncompetitively inhibited [3H]norepinephrine uptake. Propofol inhibited [3H]desipramine binding with a potency similar to that observed in [3H]norepinephrine uptake. Scatchard analysis showed that propofol competitively inhibited [3H]desipramine binding. On the other hand, long-term treatment of cells with propofol (10 microm) enhanced the NET functional activity and [3H]desipramine binding, and also increased the level of NET mRNA. Conclusions These results suggest that intravenous anesthetics have a dual effect on NET; short-term treatment causes inhibition, whereas long-term treatment leads to up-regulation. The interaction of intravenous anesthetics with NET may modulate the neuronal transmission of norepinephrine during anesthesia.

Ketamine interacts with the noradrenaline transporter at a site partly overlapping the desipramine binding site

1998 ◽  
Vol 358 (3) ◽  
pp. 328-333 ◽  
Author(s):  
Koji Hara ◽  
N. Yanagihara ◽  
Kouichiro Minami ◽  
Susumu Ueno ◽  
Yumiko Toyohira ◽  
...  
Keyword(s):  
Binding Site ◽  
Noradrenaline Transporter ◽  
Desipramine Binding ◽  
A Site
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