Literature DB >> 17766108

Antinociceptive activity of furan-containing congeners of improgan and ranitidine.

L B Hough1, W M P B Menge, A C van de Stolpe, J W Nalwalk, R Leurs, I J P de Esch.   

Abstract

Furan-containing congeners of the histamine H(2) receptor antagonist ranitidine were synthesized and tested for improgan-like antinociceptive activity. The most potent ligand of the series, VUF5498, is the most potent improgan-like agent described to date (ED(50)=25 nmol, icv). This compound is approximately equal in potency with morphine. These non-imidazole, improgan-like pain relievers further define the structural requirements for analgesics of this class and are important tools for ongoing mechanism-based studies.

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Year:  2007        PMID: 17766108      PMCID: PMC2094356          DOI: 10.1016/j.bmcl.2007.07.060

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  13 in total

1.  Activation of brain stem nuclei by improgan, a non-opioid analgesic.

Authors:  J W Nalwalk; K Svokos; O Taraschenko; R Leurs; H Timmerman; L B Hough
Journal:  Brain Res       Date:  2004-09-24       Impact factor: 3.252

2.  Antinociceptive activity of derivatives of improgran and burimamide.

Authors:  L B Hough; J W Nalwalk; R Leurs; W M Menge; H Timmerman
Journal:  Pharmacol Biochem Behav       Date:  2000-01-01       Impact factor: 3.533

3.  Cannabinoid-improgan cross-tolerance: Improgan is a cannabinomimetic analgesic lacking affinity at the cannabinoid CB1 receptor.

Authors:  Julia W Nalwalk; Konstantina Svokos; Lindsay B Hough
Journal:  Eur J Pharmacol       Date:  2006-08-26       Impact factor: 4.432

4.  Novel qualitative structure-activity relationships for the antinociceptive actions of H2 antagonists, H3 antagonists and derivatives.

Authors:  L B Hough; J W Nalwalk; B Y Li; R Leurs; W M Menge; H Timmerman; M E Carlile; C Cioffi; M Wentland
Journal:  J Pharmacol Exp Ther       Date:  1997-12       Impact factor: 4.030

5.  Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.

Authors:  Herman D Lim; Richard M van Rijn; Ping Ling; Remko A Bakker; Robin L Thurmond; Rob Leurs
Journal:  J Pharmacol Exp Ther       Date:  2005-06-09       Impact factor: 4.030

6.  Cloning, expression, and pharmacological characterization of a novel human histamine receptor.

Authors:  Y Zhu; D Michalovich; H Wu; K B Tan; G M Dytko; I J Mannan; R Boyce; J Alston; L A Tierney; X Li; N C Herrity; L Vawter; H M Sarau; R S Ames; C M Davenport; J P Hieble; S Wilson; D J Bergsma; L R Fitzgerald
Journal:  Mol Pharmacol       Date:  2001-03       Impact factor: 4.436

7.  Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.

Authors:  Timothy A Esbenshade; Kathleen M Krueger; Thomas R Miller; Chae Hee Kang; Lynne I Denny; David G Witte; Betty B Yao; Gerard B Fox; Ramin Faghih; Youssef L Bennani; Michael Williams; Arthur A Hancock
Journal:  J Pharmacol Exp Ther       Date:  2003-02-20       Impact factor: 4.030

8.  Antinociceptive effect of centrally administered cimetidine and dimaprit in the rat.

Authors:  C Netti; R Bossa; I Galatulas; V Sibilia; A Pecile
Journal:  Pharmacology       Date:  1984       Impact factor: 2.547

9.  The disposition of thioperamide, a histamine H3-receptor antagonist, in rats.

Authors:  E Sakurai; E Gunji; Y Iizuka; N Hikichi; K Maeyama; T Watanabe
Journal:  J Pharm Pharmacol       Date:  1994-03       Impact factor: 3.765

10.  Characterization of the antinociceptive properties of cimetidine and a structural analog.

Authors:  B Y Li; J W Nalwalk; L A Barker; P Cumming; M E Parsons; L B Hough
Journal:  J Pharmacol Exp Ther       Date:  1996-02       Impact factor: 4.030

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  3 in total

1.  Neural basis for improgan antinociception.

Authors:  M M Heinricher; M E Martenson; J W Nalwalk; L B Hough
Journal:  Neuroscience       Date:  2010-05-24       Impact factor: 3.590

2.  Antinociceptive activity of CC44, a biotinylated improgan congener.

Authors:  Paul Hoerbelt; Julia W Nalwalk; James G Phillips; Mark P Wentland; Zhixing Shan; Lindsay B Hough
Journal:  Eur J Pharmacol       Date:  2013-07-05       Impact factor: 4.432

3.  Non-opioid antinociception produced by brain stem injections of improgan: significance of local, but not cross-regional, cannabinoid mechanisms.

Authors:  Lindsay B Hough; Konstantina Svokos; Julia W Nalwalk
Journal:  Brain Res       Date:  2008-10-21       Impact factor: 3.252

  3 in total

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