| pubmed-article:10991982 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:10991982 | lifeskim:mentions | umls-concept:C0597357 | lld:lifeskim |
| pubmed-article:10991982 | lifeskim:mentions | umls-concept:C0243192 | lld:lifeskim |
| pubmed-article:10991982 | lifeskim:mentions | umls-concept:C0033262 | lld:lifeskim |
| pubmed-article:10991982 | lifeskim:mentions | umls-concept:C0003209 | lld:lifeskim |
| pubmed-article:10991982 | lifeskim:mentions | umls-concept:C0019588 | lld:lifeskim |
| pubmed-article:10991982 | lifeskim:mentions | umls-concept:C1515999 | lld:lifeskim |
| pubmed-article:10991982 | lifeskim:mentions | umls-concept:C0871161 | lld:lifeskim |
| pubmed-article:10991982 | lifeskim:mentions | umls-concept:C0540496 | lld:lifeskim |
| pubmed-article:10991982 | pubmed:issue | 1 | lld:pubmed |
| pubmed-article:10991982 | pubmed:dateCreated | 2000-11-3 | lld:pubmed |
| pubmed-article:10991982 | pubmed:abstractText | BP 2-94 is an azomethine prodrug of (R)-alpha-methylhistamine [(R)-alpha-MeHA], a potent and selective histamine H(3)-receptor agonist. When administered orally to mice BP 2-94 was distributed to various peripheral tissues where it released the active drug. BP 2-94 displayed anti-inflammatory and antinociceptive properties in mice. It dose-dependently inhibited carrageenan-induced paw edema with an ED(50) value of 0.17 +/- 0.05 micromol/kg (p.o.) and a maximal effect of 47%. It also reduced Freund's complete adjuvant-induced paw edema in preventive as well as in curative fashion. Repeated oral administrations of BP 2-94 reduced the pre-established Freund's complete adjuvant-induced edema with an ED(50) value of 5 +/- 2 micromol/kg (p.o.) and a maximal effect of 47%. The antiedema effects of BP 2-94 and indomethacin were additive. BP 2-94 was also efficient in reducing cyclophosphamide-induced cystitis in mice: it decreased leukocyte infiltration by 62% and plasma protein extravasation by 73% in urinary bladder. In addition, BP 2-94 displayed antinociceptive activity in the capsaicin-induced licking test via H(3)-receptor stimulation. Its antinociceptive effect was dose dependent, occurring with an ED(50) value of 0.4 +/- 0.1 micromol/kg (p.o.) and a maximal reduction of licking duration by 69%. No tolerance to the antinociceptive effect was observed after repeated administration of BP 2-94 for 3 days. These observations with BP 2-94 suggest that H(3)-receptor agonists might represent a novel class of anti-inflammatory and antinociceptive agents. | lld:pubmed |
| pubmed-article:10991982 | pubmed:language | eng | lld:pubmed |
| pubmed-article:10991982 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10991982 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:10991982 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10991982 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:10991982 | pubmed:month | Oct | lld:pubmed |
| pubmed-article:10991982 | pubmed:issn | 0022-3565 | lld:pubmed |
| pubmed-article:10991982 | pubmed:author | pubmed-author:SchunackWW | lld:pubmed |
| pubmed-article:10991982 | pubmed:author | pubmed-author:SchwartzJ CJC | lld:pubmed |
| pubmed-article:10991982 | pubmed:author | pubmed-author:StarkHH | lld:pubmed |
| pubmed-article:10991982 | pubmed:author | pubmed-author:RouleauAA | lld:pubmed |
| pubmed-article:10991982 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:10991982 | pubmed:volume | 295 | lld:pubmed |
| pubmed-article:10991982 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:10991982 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:10991982 | pubmed:pagination | 219-25 | lld:pubmed |
| pubmed-article:10991982 | pubmed:dateRevised | 2003-11-14 | lld:pubmed |
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| pubmed-article:10991982 | pubmed:year | 2000 | lld:pubmed |
| pubmed-article:10991982 | pubmed:articleTitle | Anti-inflammatory and antinociceptive properties of BP 2-94, a histamine H(3)-receptor agonist prodrug. | lld:pubmed |
| pubmed-article:10991982 | pubmed:affiliation | Unité de Neurobiologie et Pharmacologie Moléculaire (U.109) de l'Institut National de la Santé et de la Recherche Médicale, Centre Paul Broca, Paris, France. rouleau@broca.inserm.fr | lld:pubmed |
| pubmed-article:10991982 | pubmed:publicationType | Journal Article | lld:pubmed |
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