Three behavioral models were used to characterize the pharmacological action of BCH 325 on central dopaminergic transmission. The effect of acute SC treatment with BCH 325 upon dopaminergic mechanisms affecting motor activity was studied on the climbing behavior of mice. It was shown that the beta-casomorphin analogue evoked a dose-dependent increase in apomorphine (APO)-induced hypoactivity that was reversed by sulpiride (SULP). In in vitro studies on slices of nucleus accumbens of mice it could be demonstrated that 10(-6) M APO caused a reduction of K(+)-stimulated [14C]dopamine (DA) release that was potentiated following simultaneous incubation with 10(-6) M BCH 325. To prove a postsynaptic influence in D1 receptor-mediated behavior pattern, the action of BCH 325 was studied on bromocriptine (BROMO)-evoked yawning behavior of rats after pretreatment with reserpine (RES) or saline. The peptide could not influence the BROMO yawning after saline administration, but it was able to normalize the number of yawns, which were reduced after RES. To investigate the effect of BCH 325 on postsynaptic D2 receptors, jerking behavior on RES-pretreated rats after a high dose of BROMO was used. Following RES pretreatment only, the number of BROMO-induced jerks was decreased by treatment of rats with 0.5 mumol/kg BCH 325. In contrast, the jerking behavior was enhanced by 0.5 mumol/kg BCH 325 in rats that were additionally treated with alpha-methyl-p-tyrosine (MPT). In biochemical studies on slices of the nucleus accumbens of mice, the in vivo pretreatment with RES caused a reduction of K(+)-stimulated [14C]DA release that was blocked by the SC administration of 0.5 mumol/kg BCH 325.(ABSTRACT TRUNCATED AT 250 WORDS)

1994-01-01·Peptides3区 · 医学

Effects of [des-Tyr-d-Phe3]beta-casomorphin (2–5) on cortical EEG power spectra in rats

3区 · 医学

Article

作者: Schulz, Stefan ; Wetzel, Wolfram ; Diedrich, Michael

The effects of the peptide [des-Tyr-D-Phe3]beta-casomorphin(2-5) (BCH-325; Pro-D-Phe-Pro-Gly; 2.27, 22.7, and 227 micrograms/kg) on cortical EEG power spectra in rats were studied compared to those of other psychotropic drugs, including diazepam, amitriptyline, haloperidol, and amphetamine. All drugs were injected IP, and cortical EEG power spectra were recorded from freely moving rats for 2 h postinjection. Administration of 22.7 and 227 micrograms/kg BCH-325 resulted in an increase in alpha-2 and beta-1 frequency bands and a decrease in slower frequencies (delta, theta). Our findings show that the effects of BCH-325 on cortical EEG power spectra differ from those of other psychotropic drugs.

1994-01-01·Peptides3区 · 医学

Effects of the peptide BCH-325 upon the efficacy of common antiepileptic drugs

3区 · 医学

Article

作者: Axel Becker ; Christian Ostner ; Gisela Grecksch ; Birgit Piönnigs

It was shown that BCH-325 (Pro-D-Phe-Pro-Gly), a des-tyrosine derivative of beta-casomorphin, exhibits anticonvulsive effects. In the present study, we combined the peptide with clinically used antiepileptic drugs (phenytoine, carbamazepine, diazepam, phenobarbital, and dipropyl acetate) to investigate possible interactions and, moreover, to draw conclusions concerning the mode of action of BCH-325. There were no interactions with phenytoine and carbamazepine, which might be interpreted to mean that BCH-325 exerted no action on sodium channels. The efficacy of the combinations with the other drugs (diazepam, phenobarbital, dipropyl acetate) was increased. The data suggest that the anticonvulsant effect of BCH-325 might occur by interference with elements of GABA/benzodiazepinergic neurotransmission.

100 项与 BCH-325 相关的药物交易

登录后查看更多信息