Detail of "466-97-7"

Reference

Opioid receptor sub-types involved in the control of transmitter release in cortex of the brain of the rat

Opioid receptor sub-types involved in the control of transmitter release in cortex of the brain of the rat. Hagan, R. M.; Hughes, I. E. (Dep. Pharmacol., Univ. Leeds, Leeds/Yorkshire LS2 9JT, UK). Neuropharmacology, 23(5), 491-5 (English) 1984. CODEN: NEPHBW. ISSN: 0028-3908. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) Elec. stimulation (3 Hz, 2 ms duration, 5-12 V for 2 min every 20 min) of rat cortical slices previously incubated with 3H-labeled noradrenaline [51-41-2], evoked a release of 3H which was inhibited by morphine [57-27-2], normorphine [466-97-7], Tyr-D-Ala-Gly-(N-Me)Phe-NH(CH2)2OH (RX783006) [78123-71-4], and [D-Ala2,D-Leu5]-enkephalin [63631-40-3]. Naloxone did not affect the release of 3H when given alone but antagonized the actions of the opioids, giving an equil. dissocn. const. (Ke) value of ~3 nM regardless of the particular agonist used, which suggests an action at m receptors. The d-opioid receptor blocker, ICI 154129, antagonized the opioids only in large concns. (Ke 21,300 nM). In slices previously incubated with 3H-labeled 5-hydroxytryptamine [50-67-9], elec. stimulation increased overflow of 3H but neither naloxone nor the opioid agonists affected evoked overflow of 3H at concns. which were effective in slices incubated with [3H]noradrenaline. Apparently, stimulation of m-opioid receptors may inhibit release of noradrenaline from central noradrenergic neurons, and these receptors are not present in significant nos. in neurons releasing 5-hydroxytryptamine in the cortex.

Effect of pertussis toxin on normorphine-dependence and on acute inhibitory effects of normorphine and clonidine in guinea pig isolated ileum

Effect of pertussis toxin on normorphine-dependence and on acute inhibitory effects of normorphine and clonidine in guinea pig isolated ileum. Tucker, J. F. (Dep. Pharmacol., Chelsea Coll., London SW3 6LX, UK). Br. J. Pharmacol., 83(2), 326-8 (English) 1984. CODEN: BJPCBM. ISSN: 0007-1188. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) In ileum isolated from guinea pigs pretreated with Pertussis toxin, the acute inhibitory effects of normorphine [466-97-7] and clonidine [4205-90-7] on elec. induced contractions were markedly attenuated while responses to acetylcholine and elec. stimulation were unaltered. Pertussis toxin treatment also reduced naloxone-pptd. withdrawal contractures in normorphine-dependent tissues. These results suggest that the acute and chronic effects of normorphine are mediated by the same mechanism, namely that of adenylate cyclase [9012-42-4] inhibition.