Detail of "80125-14-0"

Reference

The application of numerical convolution and deconvolution on different dosage forms of remoxipride

The application of numerical convolution and deconvolution on different dosage forms of remoxipride. Nicklasson, M.; Graffner, C.; Nilsson, M. I.; Wahlen, A. (Res. Dev. Lab., Astra Laekemedel AB, Soedertaelje S-151 85, Swed.). Biopharm. Pharmacokinet., Eur. Congr., 2nd, Volume 1, 124-31. Edited by: Aiache, J. M.; Hirtz, J. Lavoisier: Paris, Fr. (English) 1984. CODEN: 53JFAA. DOCUMENT TYPE: Conference CA Section: 63 (Pharmaceuticals) The absorption properties of remoxipride (I) [80125-14-0] were investigated in 2 sep. studies in healthy volunteers. The absorption after administration of an oral soln. was studied by means of numerical deconvolution and the process was completed after 2 h. Predicted plasma concn.-time curves were calcd. for different I tablets, and were close to the obsd. mean ones. The rate of absorption was soln. rate-limited. The amt. dissolved in vitro was correlated well with the amt. dissolved in vivo.

Remoxipride, a new potential antipsychotic compound with selective anti-dopaminergic actions in the rat brain

Remoxipride, a new potential antipsychotic compound with selective anti-dopaminergic actions in the rat brain. Oegren, S. O.; Hall, H.; Koehler, C.; Magnusson, O.; Lindbom, L. O.; Aengeby, K.; Florvall, L. (Dep. Pharmacol., Astra Laekemedel AB, Sodertalje S-151 85, Swed.). Eur. J. Pharmacol., 102(3-4), 459-74 (English) 1984. CODEN: EJPHAZ. ISSN: 0014-2999. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 2 The antidopaminergic actions of remoxipride (I) [80125-14-0] were detd. in rats. I preferentially blocked apomorphine-induced hyperactivity with weak effects on stereotypies. The potency of I was ~50 times higher than that of sulpiride. I caused a weak, atypical form of catalepsy and showed a high sepn. between the ED50 for blockade of apomorphine-induced hyperactivity and the ED50 for induction of catalepsy (ratio 24). I was a selective dopaminergic D2 receptor antagonist since it displaced [3H]spiperone, but not [3H]flupenthixol, in rat striatum, and did not inhibit striatal dopamine (DA) [51-61-6]-sensitive adenylate cyclase in vitro. I was a potent antagonist of D2 receptors, showing a dose-dependent blockade of [3H]spiperone and [3H]n-propylnorapomorphine in vivo binding with a potency equal to that of chlorpromazine. In contrast to haloperidol, I caused a preferential blockade of in vivo [3H]spiperone binding in the mesolimbic DA rich areas and the substantia nigra with much less effect in the striatum. In addn., I produced a preferential increase of DA utilization following synthesis inhibition in the olfactory tubercle. Only minor changes in noradrenaline and 5-hydroxytryptamine metab. were obsd., whereas homovanillic acid [306-08-1] and DOPAC [102-32-9] levels were markedly elevated. I apparently is a potent, selective D2 receptor blocking agent with a preferential action in mesolimbic and extrastriatal DA-contg. neurons.