The pharmacology of sibutramine hydrochloride (BTS 54 524), a new antidepressant which induces rapid noradrenergic down-regulation

@article{Buckett1988ThePO,
  title={The pharmacology of sibutramine hydrochloride (BTS 54 524), a new antidepressant which induces rapid noradrenergic down-regulation},
  author={W. Roger Buckett and P. C. Thomas and Graham P. Luscombe},
  journal={Progress in Neuro-Psychopharmacology and Biological Psychiatry},
  year={1988},
  volume={12},
  pages={575-584}
}
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132 Citations
Highly Influential Citations
1
Background Citations
24
Methods Citations
1
Results Citations
3

132 Citations

Antidepressant treatments, including electroconvulsive shock and the putative antidepressant sibutramine hydrochloride, do not alter [3H]-prazosin binding to rat cortical membranes

Treatment for 1, 3 or 10 days with sibutramine hydrochloride, desi pramine, amitriptyline, or pargyline did not effect the number or affinity of α1-adrenoceptors as determined by [3H]-prazosin binding to rat cerebral cortical membranes.

The contribution of metabolites to the rapid and potent down-regulation of rat cortical β-adrenoceptors by the putative antidepressant sibutramine hydrochloride

Effects of sibutramine on anxiety-related behaviours in rats.

Absence of sibutramine effect on spontaneous anxiety in rats.

The acute and chronic administration of sibutramine is not related to anxiolytic or anxiogenic effects, and the maximum effect of anti-obesity in rats, did not interfere with anxiety.

A comparison of various antidepressant drugs demonstrates rapid desensitisation of α2-adrenoceptors exclusively by sibutramine hydrochloride

This comparative study using antidepressant treatments with differing pharmacological modes of action demonstrated that sibutramine was the only drug which rapidly down-regulated pre- and postsynaptic α2-adrenoceptors.

Sibutramine. A review of its contribution to the management of obesity.

Obese patients with type 2 (non-insulin-dependent) diabetes or hypertension lost significantly more mean bodyweight with sibutramine than with placebo, although weight loss was less than that in obese patients without comorbidities, and concerns over potential pressor effects are reflected in the manufacturer's dosage and administration recommendations.

Thermogenic effects of sibutramine and its metabolites

The thermogenic activity of the serotonin and noradrenaline reuptake inhibitor sibutramine (BTS 54524; Reductil) was investigated by measuring oxygen consumption (VO2) in rats treated with…

Abuse liability assessment of sibutramine, a novel weight control agent

Data indicate sibutramine lacks amphetamine-type abuse liability when administered acutely, and is likely to have low abuse potential when administered in the therapeutic range.

Sibutramine: a novel new agent for obesity treatment.

Sibutramine, 5 and 20 mg/day, produced a dose-related weight loss in obese subjects compared to placebo in an 8-week trial and shows promise as an antiobesity drug.

Investigation of the mechanisms underlying the hypophagic effects of the 5‐HT and noradrenaline reuptake inhibitor, sibutramine, in the rat

1 Sibutramine is a novel 5‐hydroxytryptamine (5‐HT) and noradrenaline reuptake inhibitor (serotonin‐ noradrenaline reuptake inhibitor, SNRI) which is currently being developed as a treatment for…
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References

SHOWING 1-6 OF 6 REFERENCES

BTS 54 524—an Approach to a Rapidly Acting Antidepressant

Since the tricyclic antidepressant drugs were first introduced into therapy, consistent efforts have been made to improve upon their effects in terms of both increased efficacy and reduced side-effects, but the wide-spectrum monoamine uptake inhibitors still remain the most widely used drugs for the treatment of depression.

Problems with current catecholamine hypotheses of antidepressant agents: Speculations leading to a new hypothesis

  • E. Stone
  • Psychology, Biology
    Behavioral and Brain Sciences
  • 1983
A new formulation, the output hypothesis, which is derived from the foregoing theories, is proposed, and assumes that depression or adverse behavioral effects of stress results when the output of brain cells bearing noradrenergic receptors is too low to meet increased demand resulting from stress or other biologically disruptive events.

Antipsychotic medication: clinical guidelines for maintenance therapy.

  • J. Da
  • Psychology, Medicine
  • 1985
Results are summarized from studies regarding drug therapy in conjunction with psychotherapeutic factors and family environment, the efficacy of lower dosage, benefit/risk ratios, and the advantages of long-term neuroleptic maintenance.

The noradrenergic cyclic AMP generating system in the limbic forebrain: pharmacological characterization in vitro and possible role of limbic noradrenergic mechanisms in the mode of action of antipsychotics.

STUDIES IN VIVO ON THE RELATIONSHIP BETWEEN BRAIN TRYPTOPHAN, BRAIN 5‐HT SYNTHESIS AND HYPERACTIVITY IN RATS TREATED WITH A MONOAMINE OXIDASE INHIBITOR AND L‐TRYPTOPHAN

It is suggested that when monoamine oxidase is inhibited and the rate of 5‐HT synthesis is increased, granular uptake and storage of 5-HT and other rate‐limiting mechanisms for 5‐ht inactivation are unable to prevent 5‐ HT 'spilling over’ to produce hyperactivity.

Bioassay of Rauwolfia roots and alkaloids.