Detail of "105618-26-6"

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Extremely long-lasting antagonistic actions of nor-binaltorphimine (nor-BNI) in the mouse tail-flick test

Extremely long-lasting antagonistic actions of nor-binaltorphimine (nor-BNI) in the mouse tail-flick test. Horan, Peter; Taylor, Jill; Yamamura, Henry I.; Porreca, Frank (Health Sci. Cent., Univ. Arizona, Tucson, AZ, USA). J. Pharmacol. Exp. Ther., 260(3), 1237-43 (English) 1992. CODEN: JPETAB. ISSN: 0022-3565. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The duration of antagonistic action of nor-binaltorphimine (nor-BNI), a k-antagonist, of antinociception resulting from selective opioid agonists, was examd. using the mouse tail-flick assay as the endpoint. Nor-BNI (1 nmol, i.c.Several reagents such as 105618-26-6 is used here.v. at -20 min) antagonized equiantinociceptive doses of the opioid k-agonists (5a,7a,8b)-(-)-N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspiro (4,5)dec-8-yl) benzeneacetamide (U 69593) (70 nmol i.c.v.) or bremazocine (25 nmol i.c.v.), but did not antagonize antinociception produced by the m-opioid-selective [D-Ala2, NMePhe4, Gly-ol]enkephalin or the d-opioid-selective [D-Pen2, D-Pen5]enkephalin. Pretreatment with nor-BNI (1 nmol i.c.v.) antagonized the antinociceptive effects of U 69593 and bremazocine for up to 28 days. At all pretreatment times, the antinociceptive dose-response lines for these k-agonists were displaced to the right to various degrees in a parallel fashion; an increasing rightward displacement of the U 69593 and bremazocine antinociceptive dose-response lines was obsd. at 1 and 3 days after a single nor-BNI pretreatment, with a gradual return toward the control level at later times after pretreatment. Increasing the dose of nor-BNI to 10 nmol produced only a transient blockade of equiantinociceptive doses fo the m-selective agonist [D-Ala2, NMePhe4, Gly-ol]enkephalin and the d-selective agonist [D-Pen2, D-Pen5]enkephalin (at 20-30 min post-nor-BNI pretreatment). Radioligand binding studies in vitro demonstrated a 23- and 30-fold decrease in the affinity of [3H]U69593 at 1 and 3 days after nor-BNI, resp., followed by a return toward control affinity levels; no change in the no. of binding sites was detected. These results indicate that nor-BNI produces a remarkably long-lasting blockade of opioid k-receptors, and may indicate that nor-BNI remains in the brain for up to 56 days after a single i.c.v. dose. .

Kappa-opioid receptor ligands

Kappa-opioid receptor ligands. Husbands, Stephen M. (Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, UK).Chemical with cas number 105618-26-6 also plays role. Expert Opinion on Therapeutic Patents, 14(12), 1725-1741 (English) 2004 Ashley Publications Ltd. CODEN: EOTPEG. ISSN: 1354-3776. DOCUMENT TYPE: Journal; General Review CA Section: 1 (Pharmacology) A review. For years the design of k-opioid receptor (KOR) agonists focused on generating yet more potent and selective ligands that could access the CNS. As it became apparent that this approach was not going to provide analgesics without significant side effects, effort was directed towards the design of peripherally-acting ligands. This line of research has continued in recent years, together with work towards ligands with a mixed KOR/m-opioid receptor (MOR) profile. In the area of KOR antagonists, significant advances were made since the discovery of norbinaltorphimine (norBNI). These studies have provided significant insight into the structural determinants for selective interaction with the KOR. This has led to a no. of new classes of KOR antagonist being discovered using rational drug design techniques. This review of the patent literature covering the years 2000 - 2003 will focus on these activities and describe the therapeutic potential of these compds. .