Biomedical subjects

J Maj

Publications and source records attributed to J Maj.

219 records · Page 13Linked to original sources

PubMedDate not supplied

Some behavioral effects of 1,3-di-o-tolylguanidine, opipramol and sertraline, the sigma site ligands.

1,3-Di-o-tolylguanidine (DTG), opipramol (OPI) and sertraline (SER), sigma site ligands, were studied in Wistar rats and Albino Swiss mice, mainly with regard to their interaction with dopamine drugs. DTG and SER (at the highest doses only) decreased the spontaneous locomotor activity. DTG did not change the amphetamine locomotor hyperactivity, while OPI and SER decreased it. The amphetamine stereotypy was slightly increased (prolonged) by all the three drugs. OPI antagonized the locomotor hyperactivity, stereotypy, aggression and climbing, all those being induced by apomorphine; DTG inhibited only the aggression, while SER-the aggression and climbing (the latter was also inhibited by paroxetine, which showed no affinity for sigma sites). DTG and SER (but not paroxetine) were able to increase the locomotor hyperactivity induced by quinpirole. That effect was antagonized by OPI which-when given alone-did not affect the quinpirole hyperlocomotion. The reserpine-induced akinesia was not affected by DTG, OPI or SER; the L-DOPA hyperactivity in reserpinized rats was changed (increased) by DTG only. DTG and SER (also paroxetine and citalopram), but not OPI, increased the cocaine locomotor hyperactivity. All the three sigma ligands given alone did not evoke catalepsy; the haloperidol- and spiperone-induced catalepsy was attenuated by DTG and OPI, but increased by SER. The MK-801-induced hyperactivity was decreased by DTG, but increased by OPI and SER. In the forced swimming test, only DTG slightly reduced the immobility time; the reduction of the immobility time induced by MK-801 was not changed by DTG, but increased by OPI and SER. Only DTG evoked a dose-dependent decrease in the body temperature, which was not changed by rimcazole. The above results indicate that the sigma site ligands studied differ in their pharmacological profile; however, it is still difficult to determine unequivocally whether they show agonistic or antagonistic properties.

1-Naphthylamine↗

PubMedDate not supplied

Locomotor activity and motor disturbances induced by the competitive NMDA receptor antagonist CGP 37849.

The study compares the effects of the competitive NMDA receptor antagonist, CGP 37849, on the locomotor activity and motor disturbances after local, unilateral microinjection into nucleus accumbens and caudateputamen or peripheral ip administration. Independently on the route of administration, the compound induced dose-dependent increase in the locomotor activity as well as the symptoms of motor disturbances. In all cases the symptoms of motor disturbances appeared earlier and lasted longer than increase in locomotor activity induced by the same dose of the drug. The long-lasting observation indicated, that CGP 37849 administered in a dose of 20 mg/kg ip increased the locomotor activity of the rats for about 2 h while motor disturbances persisted for about 6 h. Administration of the lowest dose of CGP 37849, i.e. 0.05 microgram into the nucleus accumbens, or 10 mg/kg ip-while without any effect on the locomotor activity-induced the symptoms of motor disturbances. Pretreatment with SKF-525-A (proadifen, an agent inhibiting the metabolism of the drugs), fully antagonized the locomotor hyperactivity induced by CGP 37849 given in a dose of 20 mg/kg, and-in the same time-diminished the degree of motor disturbance symptoms. On the other hand, in the case of the dose of 10 mg/kg of CGP 37849, SKF-525-A did not affect the locomotor activity, but enhanced the motor disturbance symptoms induced by this dose of CGP 37849. In conclusion, the obtained results indicate that CGP 37849 administered peripherally or locally to the brain regions cited above induces motor disturbances at doses lower (or at least similar) than these which stimulate the locomotor activity.

2-Amino-5-phosphonovalerate↗

PubMedDate not supplied

Pharmacological profile of venlafaxine, a new antidepressant, given acutely.

Pharmacological effects of acute treatment with venlafaxine (VEN), a clinically active antidepressant [a noradrenaline (NA) and 5-hydroxytryptamine (5-HT) reuptake inhibitor without any affinity for neurotransmitter receptors] were studied in mice and rats. VEN inhibited the reserpine- or apomorphine-induced hypothermia and enhanced the L-5-HTP-induced head twitches in mice. It reduced the immobility time in Porsolt's test in mice and rats, but either did not change the locomotor activity (mice) or decreased it (rats). VEN reduced the locomotor hyperactivity induced by amphetamine (AMP), apomorphine (APO) and quinpirole (QUI), as well as the APO-induced stereotypy; the stereotypy induced by AMP in rats was prolonged. VEN neither changed the clonidine-induced aggressiveness in mice nor the behavioral syndrome induced by oxotremorine in rats. The obtained results indicate that VEN, given acutely, shows a pharmacological profile similar to that of tricyclic NA and 5-HT reuptake inhibitors. In contrast to the antidepressants mentioned above, VEN does not exhibit an alpha 1-adrenolytic or a cholinolytic activity (in vivo tests).

Aggression↗