Specific tricyclic antidepressant binding sites in rat brain characterised by high-affinity 3H-imipramine binding

Raisman, Rita; Briley, Mike; Langer, Salomón Z.

doi:10.1016/0014-2999(80)90076-x

Cited by 245 publications

(56 citation statements)

References 21 publications

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“…Venlafaxine 030) is a novel non-tricyclic compound (1-2-(dimethylamino)-1-(4-methoxyphenyl)ethyl cyclohexanol, hydrochloride) (Husbands et al, 1985) which has in vitro and in vivo pharmacological activity similar to the tricyclic antidepressants Raisman et al, 1980). It inhibits neuronal uptake of serotonin, noradrenaline and dopamine in order of decreasing potency (Muth et al, 1986).…”

Section: Introductionmentioning

confidence: 99%

Pharmacodynamics of venlafaxine evaluated by EEG brain mapping, psychometry and psychophysiology.

Saletu

Grünberger

Anderer

et al. 1992

Brit J Clinical Pharma

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1 In a double-blind, placebo-controlled study the effects of venlafaxine-a novel nontricyclic compound inhibiting neuronal uptake of serotonin, noradrenaline and to a lesser extent dopamine -were investigated utilizing EEG brain mapping, psychometric and psychophysiological measures. 2 Sixteen healthy volunteers (eight males, eight females) aged 21-36 years received randomized and at weekly intervals single oral doses of placebo, 12.5 mg, 25 mg and 50 mg venlafaxine. EEG recordings, psychometric and psychophysiological tests, and evaluation of pulse, blood pressure and side-effects were carried out at 0, 2, 4, 6, and 8 h. 3 EEG brain mapping demonstrated that venlafaxine exerted a significant action on human brain function as compared with placebo at all three doses, characterized mostly by attenuation of absolute power, increase of relative delta/theta and beta, and decrease of alpha power, as well as by an acceleration of the total centroid frontotemporally and by its slowing centrally and parietally. These findings are similar to antidepressants such as imipramine. Topographically, drug-induced alterations were most pronounced over both fronto-temporal and the right temporal to temporooccipital regions. 4 Psychometric and psychophysiological investigations demonstrated significant dosedependent psychotropic properties of the drug. Multivariate statistics exhibited an improvement of both the noopsyche (e.g. attention, concentration, attention variability, memory, fine motor activity, reaction time performance) and thymopsyche (e.g. drive, wakefulness)) but also significant psychophysiological activation (e.g. in c.f.f., pupillary and skin conductance measures). 5 Time-efficiency calculations showed significant central effects from the 2nd hour onwards, with increasing differences between placebo and treatment up to the 8th hour. Nausea was the most frequent complaint and appeared dose dependent.

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Section: Introductionmentioning

confidence: 99%

Pharmacodynamics of venlafaxine evaluated by EEG brain mapping, psychometry and psychophysiology.

Saletu

Grünberger

Anderer

et al. 1992

Brit J Clinical Pharma

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“…On the other hand, 5-methoxy tryptamine showed a higher inhibitory effect than that of tryptamine. In the solubilized DA receptors from rat striatum, Gorissen et al We have demonstrated the presence of high affinity 3H-imipramine binding sites by a theoretical kinetic analysis (16) in addition to the reports based on the displacement method by unlabelled imipramine (21)(22)(23). From these evidences, the tryptamine binding mode was examined by a theoretical kinetic treatment.…”

Section: Discussionmentioning

confidence: 98%

Butanol extracts from myelin fragements: some characteristics of tryptamine binding.

et al. 1982

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Abstract-Myelin fragments from rat brain stems were treated with butanol water mixtures and binding experiments of 14C-tryptamine to these extracts (i.e. proteolipids) were performed by Sephadex LH20 column chromato graphy. The elution peak of 14C-tryptamine appeared in a boundary between 6:1 and 4:1 chloroform-methanol, together with 19.2 and 7.3% of the total recoveries of protein and lipid phosphorus, respectively. Various compounds were studied to examine their inhibitory effects on the tryptamine binding to these extracts. The results indicated that only tryptamine and 5-methoxytryptamine inhibited the tryptamine binding, but indole analogues and other neurotransmitters had no effect. The kinetic analysis revealed that the tryptamine binding components present in the myelin butanol extracts are composed of saturable and non-saturable components, and the saturable binding components had an apparent Kd of 1.14X10-7 M. As a preliminary study, myelin butanol extracts were separated into a lipid and protein fractions with ice-cold ether treatment, and then the 14C tryptamine binding capacities of both fractions were examined. The results indicated that only the lipid fraction possessed a tryptamine binding capacity and a chromatographic profile similar to the original butanol extracts. Moreover, the heat-treated preparation of myelin extracts also retained the tryptamine binding capacity. All these observations suggest that the myelin butanol extracts have a specific binding capacity for tryptamine, and its binding components may be lipid in nature.

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“…All rats were killed 48 h after the last injection, unless specifically indicated; the entire cortex (plus hippocampus) and the corpus striatum were quickly dissected and stored at -80°C until assayed. The nuclear pellet of one cortical or two striatal homogenates for each experiment was sedimented at 900 g for 10 min; partially purified membranes were then obtained, and the binding of [3H]-imipramine 774 A. VACCARI (0.25-10 nM) was measured essentially as described by Raisman et al (1980). Membranes (200 p1u of 1:26 w/v suspension) were mixed with [3H]-imipramine in the absence or presence of 100 pM desipramine as the displacer, in 50mM Tris-HCI buffer, pH 7.5 at 4°C, containing 120mM NaCl and 5 mM KCI, and incubated in a total volume of 0.5 ml over ice for 60 min.…”

Section: Methodsmentioning

confidence: 99%

“…A diminished binding of the tricyclic antidepressant imipramine to brain and platelet putative 'receptors' has been suggested to represent a biological 'marker' for endogenous depression (Langer et al, 1981). Furthermore, [3H]-imipramine recognition sites are anatomically and functionally associated with the 5-hydroxytryptamine (5-HT) uptake mechanism (Langer et al, 1980).…”

Section: Introductionmentioning

confidence: 99%

Effects of neonatal antithyroid treatment on brain [³H]‐imipramine binding sites

Vaccari

1985

British J Pharmacology

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Specific tricyclic antidepressant binding sites in rat brain characterised by high-affinity 3H-imipramine binding

Cited by 245 publications

References 21 publications

Pharmacodynamics of venlafaxine evaluated by EEG brain mapping, psychometry and psychophysiology.

Pharmacodynamics of venlafaxine evaluated by EEG brain mapping, psychometry and psychophysiology.

Butanol extracts from myelin fragements: some characteristics of tryptamine binding.

Effects of neonatal antithyroid treatment on brain [³H]‐imipramine binding sites

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Specific tricyclic antidepressant binding sites in rat brain characterised by high-affinity 3H-imipramine binding

Cited by 245 publications

References 21 publications

Pharmacodynamics of venlafaxine evaluated by EEG brain mapping, psychometry and psychophysiology.

Pharmacodynamics of venlafaxine evaluated by EEG brain mapping, psychometry and psychophysiology.

Butanol extracts from myelin fragements: some characteristics of tryptamine binding.

Effects of neonatal antithyroid treatment on brain [3H]‐imipramine binding sites

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Effects of neonatal antithyroid treatment on brain [³H]‐imipramine binding sites