Tags

Type your tag names separated by a space and hit enter

Effects of naltrexone and histamine antagonists on the antinociceptive activity of the cimetidine analog SKF92374 in rats.
Brain Res. 1997 Feb 14; 748(1-2):168-74.BR

Abstract

A recent study showed that SKF92374, a structural analog of the histamine H2 receptor antagonist cimetidine, induces antinociception after intraventricular (i.v.t.) administration in the rat. SKF92374 lacked significant activity on H1 or H2 receptors, but had weak activity on H3 receptors. To test the hypothesis that SKF92374-induced antinociception is mediated by an action on H3 receptors, the effects of the H3 agonist R-alpha-methylhistamine (RAMH) and the H3 antagonist thioperamide (both by i.v.t. administration) were investigated on SKF92374 antinociception. SKF92374-induced antinociception was slightly enhanced by thioperamide (30 microg), but unaffected by a range of doses of RAMH (up to 2 microg). Furthermore, SKF92374-induced antinociception was not reduced by large doses of systemically-administered antagonists of H1 (pyrilamine), H2 (zolantidine), H3 (GT-2016), or opioid (naltrexone) receptors. These findings show that the novel compound SKF92374 induces antinociception by a non-opioid mechanism that does not utilize brain H1, H2 or H3 receptors.

Authors+Show Affiliations

Department of Pharmacology and Neuroscience, Albany Medical College, NY 12208, USA.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

9067458

Citation

Li, B Y., et al. "Effects of Naltrexone and Histamine Antagonists On the Antinociceptive Activity of the Cimetidine Analog SKF92374 in Rats." Brain Research, vol. 748, no. 1-2, 1997, pp. 168-74.
Li BY, Nalwalk JW, Hough LB. Effects of naltrexone and histamine antagonists on the antinociceptive activity of the cimetidine analog SKF92374 in rats. Brain Res. 1997;748(1-2):168-74.
Li, B. Y., Nalwalk, J. W., & Hough, L. B. (1997). Effects of naltrexone and histamine antagonists on the antinociceptive activity of the cimetidine analog SKF92374 in rats. Brain Research, 748(1-2), 168-74.
Li BY, Nalwalk JW, Hough LB. Effects of Naltrexone and Histamine Antagonists On the Antinociceptive Activity of the Cimetidine Analog SKF92374 in Rats. Brain Res. 1997 Feb 14;748(1-2):168-74. PubMed PMID: 9067458.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of naltrexone and histamine antagonists on the antinociceptive activity of the cimetidine analog SKF92374 in rats. AU - Li,B Y, AU - Nalwalk,J W, AU - Hough,L B, PY - 1997/2/14/pubmed PY - 1997/2/14/medline PY - 1997/2/14/entrez SP - 168 EP - 74 JF - Brain research JO - Brain Res VL - 748 IS - 1-2 N2 - A recent study showed that SKF92374, a structural analog of the histamine H2 receptor antagonist cimetidine, induces antinociception after intraventricular (i.v.t.) administration in the rat. SKF92374 lacked significant activity on H1 or H2 receptors, but had weak activity on H3 receptors. To test the hypothesis that SKF92374-induced antinociception is mediated by an action on H3 receptors, the effects of the H3 agonist R-alpha-methylhistamine (RAMH) and the H3 antagonist thioperamide (both by i.v.t. administration) were investigated on SKF92374 antinociception. SKF92374-induced antinociception was slightly enhanced by thioperamide (30 microg), but unaffected by a range of doses of RAMH (up to 2 microg). Furthermore, SKF92374-induced antinociception was not reduced by large doses of systemically-administered antagonists of H1 (pyrilamine), H2 (zolantidine), H3 (GT-2016), or opioid (naltrexone) receptors. These findings show that the novel compound SKF92374 induces antinociception by a non-opioid mechanism that does not utilize brain H1, H2 or H3 receptors. SN - 0006-8993 UR - https://www.unboundmedicine.com/medline/citation/9067458/Effects_of_naltrexone_and_histamine_antagonists_on_the_antinociceptive_activity_of_the_cimetidine_analog_SKF92374_in_rats_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0006-8993(96)01288-7 DB - PRIME DP - Unbound Medicine ER -