Avtor/Urednik		Krisch, I
Naslov		Vrednotenje antipsihotičnega potenciala dveh novosintetiziranih derivatov ergolina pri poskusnih živalih
Tip		monografija
Kraj izdaje		Ljubljana
Založnik		Medicinska fakulteta
Leto izdaje		1995
Obseg		str. 53
Jezik		slo
Abstrakt		The pharmacological properties of LEK-8829: 9,10-didehydro-N-methyl-N-(2-propynyl)-6-methyl-8beta-aminomethylergoline and LEK-8841: 9,10-didehydro-N-methyl-N-(2-propynyl)-2-bromo-6-methylergoline-8betha-carboxamide, new ergoline derivatives, were compared with those of haloperidol and clozapine using various behavioral tests in rats and mice and blood pressure measurements in rats. All compounds inhibited apomorphine-induced locomotor activity in rats, apomorphine-induced climbing behavior in mice and 5-hydroxyltryptophan-induced head twitches in mice and induced catalepsy in rats and in mice. LEK-8829 and clozapine, but not LEK-8841 and haloperidol, showed a certain degree of mesolimbic selectivity, i.e. they caused more potent ihibition of apomorphine-induced locomotion compared with the induction of catalepsy in rats. In the case of LEK-8829, nonspecific effects that presumably predict side effect profile, such as potentiation of pentobarbital-induced anesthesia in mice (sedation), antagonism of oxotremorine-induced tremor in mice (anticholinergic activity), spontaneous locomotor activity in mice, and noradrenaline-induced lethality in rats (sedation and hypotension), were relatively weak compared with the activities described earlier. In contrast, LEK-8841 showed nonspecific effects at the similar dose levels as dopamine antagonistic and 5-HT antagonistic effects. The results of direct measurements of the influences of both compounds on blood pressure agreed with the previously mentioned findings, i.e. LEK-8829 was relatively less Abstract truncated at 3200 characters.
Deskriptorji		CATALEPSY BEHAVIOR, ANIMAL ERGOLINES BLOOD PRESSURE ANIMALS, LABORATORY MICE RATS HALOPERIDOL CLOZAPINE