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Volumn 19, Issue 10, 2009, Pages 2766-2771

Synthesis and structure-activity relationships of phenothiazine carboxylic acids having pyrimidine-dione as novel histamine H1 antagonists

Author keywords

Antagonist; Carboxylic acid; H1; Histamine; Phenothiazine; Pyrimidine dione

Indexed keywords

AMINE; CARBOXYLIC ACID DERIVATIVE; HISTAMINE H1 RECEPTOR; HISTAMINE H1 RECEPTOR ANTAGONIST; KETOTIFEN FUMARATE; OVALBUMIN; PHENOTHIAZINE DERIVATIVE; PREDNISOLONE; PYRIMIDINE DERIVATIVE;

EID: 65349120142     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.03.124     Document Type: Article
Times cited : (41)

References (27)
  • 22
    • 65349144115 scopus 로고    scopus 로고
    • note
    • 3H]-pyrilamine in a total of 200 μl of binding buffer (50 mM Tris-HCl, pH 7.5). Nonspecific binding was determined in the presence of 1.25 μM triprolidine (Sigma). The assay mixture was incubated for 3 h at room temperature and then filtered through GF/B filters. These were washed and counted by a scintillation counter. Specific binding was calculated as the difference between total and nonspecific bindings.
  • 23
    • 65249191577 scopus 로고    scopus 로고
    • note
    • 2), dC/dt: slope of the cumulative reserver concentration (μM/s).
  • 24
    • 65349149259 scopus 로고    scopus 로고
    • note
    • Eight-week old female mice (ddY, SLC) was administered orally with various doses of compounds suspended in 0.5% methylcellulose 1 h before the intradermal injection of histamine (4 μg/site) to back skin following intravenous injections of Evans' blue solution. Thirty minutes after the injection of histamine, mice were sacrificed and the area of dye was measured.
  • 25
    • 65349083580 scopus 로고    scopus 로고
    • note
    • Eight-week old female mice (Balb/c, SLC) were sensitized by intraperitoneal injection of OVA with alum. After two weeks, compounds suspended in a 0.5% MC solution was po administered 60 min before OVA injection to the ear in OVA-sensitized mice. Ear swellings were determined at 1 h (ITR) and 24 h (LTR) after elicitation. Each column with vertical bar represents the mean ± SE of 6-7 mice.
  • 27
    • 65349108504 scopus 로고    scopus 로고
    • note
    • 2O: C, 53.77; H, 6.18; N, 11.61; S, 5.31. Found: C, 53.38; H, 5.93; N, 11.34; S, 5.31.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.