Synthesis of magnolol and honokiol derivatives and their effect against hepatocarcinoma cells.

The hepatocellular carcinoma is one of the most common malignant tumour with high level of mortality rate due to its rapid progression and high resistance to conventional chemotherapies. Thus, the search for novel therapeutic leads is of global interest. Herein, a small set of derivatives of magnolol 1 and honokiol 2, the main components of Magnolia grandiflora and Magnolia obovata, were evaluated in in vitro assay using tumoral hepatocytes.

Dopaminergic deficit and mood disorders.

The roles of serotonin and noradrenaline in the pathogenesis of mood disorders have been elucidated by numerous studies, which support the therapeutic use of tricyclic antidepressants and selective serotonin re-uptake inhibitors. The same has not occurred for dopamine, notwithstanding the fact that the crucial role of the mesolimbic dopaminergic system in behaviour has been known to researchers for many years. The objective of this article is to provide an overview of the animal data that demonstrate the importance of dopamine in animal behaviour and suggest that dopaminergic deficiency may cause a number of psychiatric symptoms in man.

Baclofen suppresses motivation to consume alcohol in rats.

Rationale: Recent studies demonstrated that treatment with the gamma-aminobutyric acid (GABA)(B) receptor agonist baclofen reduced alcohol intake in selectively bred Sardinian alcohol-preferring (sP) rats tested under the home-cage, two-bottle choice regimen.

Objectives: The present study investigated the effect of baclofen on the appetitive, rather than consummatory, aspects of alcohol ingestion in sP rats.

Methods: Rats were trained to lever-press for oral alcohol (10%, v/v) or sucrose (3%, w/v) under a fixed-ratio schedule of 4.

The GABA(B) receptor agonists baclofen and CGP 44532 prevent acquisition of alcohol drinking behaviour in alcohol-preferring rats.

Aims: The present study investigated the effect of the gamma-aminobutyric acid (GABA)(B) receptor agonists, baclofen and CGP 44532, on the acquisition of alcohol drinking behaviour in selectively bred Sardinian alcohol-preferring (sP) rats.

Methods: Baclofen [0, 1 and 3 mg/kg, intraperitoneally (i.p.

Evidence for functional CB1 cannabinoid receptor expressed in the rat thyroid.

Objective: Previous reports have shown that the Delta(9)-tetrahydrocannabinol (Delta(9)TCH), the major psychoactive cannabinoid components of marijuana, is able [corrected] to inhibit thyroid hormonal activity. The aim of this study was to characterize the CB1 functional expression in the rat thyroid by a multi-methods approach.

Methods And Results: RT-PCR was used to detect the mRNA expression of the CB1 cannabinoid receptor (17.

Stimulation of voluntary ethanol intake by cannabinoid receptor agonists in ethanol-preferring sP rats.

Rationale: Recent studies have shown that the cannabinoid CB1 receptor antagonist, SR 141716, is capable of reducing voluntary ethanol intake in rodents, suggesting the involvement of the CB1 receptor in the neural circuitry mediating the positive reinforcing properties of ethanol.

Objectives: The present study extended to the agonists the investigation on the pharmacological manipulation of ethanol intake by cannabinoid agents.

Methods: Selectively bred, Sardinian alcohol-preferring (sP) rats were offered ethanol and water under the two-bottle free choice procedure with unlimited access for 24 h/day.

GABA(B) receptor inhibition causes locomotor stimulation in mice.

The present study investigated the effect of the administration of the GABA(B) receptor antagonists, SCH 50911 [(2S)(+)-5,5-dimethyl-2-morpholineacetic acid], CGP 46381 [(3-aminopropyl)(cyclohexylmethyl)phosphinic acid] and CGP 52432 (3-[[(3,4-dichlorophenyl)methyl]amino]propyl]diethoxymethyl)phosphinic acid), on spontaneous locomotor activity in mice. All drugs were acutely administered at the doses of 10 and 30 mg/kg (i.p.