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Volumn 19, Issue 18, 2009, Pages 5486-5489

Solubilized phenyl-pyrazole ureas as potent, selective 5-HT2A inverse-agonists and their application as antiplatelet agents

Author keywords

5 HT2A; Antiplatelet; Antithrombosis

Indexed keywords

ADENOSINE DIPHOSPHATE; ANTITHROMBOCYTIC AGENT; IODINE 125; MACROGOL 400; PHENYLPYRAZOLE UREA DERIVATIVE; PIMAVANSERIN; POTASSIUM CHANNEL HERG; PYRAZOLE DERIVATIVE; SEROTONIN; SEROTONIN 2A AGONIST; SEROTONIN 2A RECEPTOR; UNCLASSIFIED DRUG; UREA DERIVATIVE; VOLINANSERIN;

EID: 68949083344     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.07.073     Document Type: Article
Times cited : (8)

References (20)
  • 12
    • 0025687562 scopus 로고    scopus 로고
    • De Clerck, F. F.; Janssen, P. A. J. Hypertens., 1990, S87.
    • De Clerck, F. F.; Janssen, P. A. J. Hypertens., 1990, S87.
  • 15
    • 0000414496 scopus 로고
    • Paquette, L. A, Ed, Wiley: New York
    • Hughes, D. L. In Organic Reactions; Paquette, L. A., Ed.; Wiley: New York, 1992; Vol. 42, pp 335-656.
    • (1992) Organic Reactions , vol.42 , pp. 335-656
    • Hughes, D.L.1
  • 16
    • 68949099282 scopus 로고    scopus 로고
    • For experimental details, see: Teegarden, B.; Jayakumar, H.; Li, H.; Strah-Pleynet, S.; Dosa, P. I. Preparation of diaryl and arylheteroaryl urea derivatives, in particular pyrazolylphenyl ureas, as 5-HT2A serotonin receptor modulators. WO2005012254, 2005.
    • For experimental details, see: Teegarden, B.; Jayakumar, H.; Li, H.; Strah-Pleynet, S.; Dosa, P. I. Preparation of diaryl and arylheteroaryl urea derivatives, in particular pyrazolylphenyl ureas, as 5-HT2A serotonin receptor modulators. WO2005012254, 2005.
  • 17
    • 68949097324 scopus 로고    scopus 로고
    • Teegarden, B.; Xiong, Y.; Strah-Pleynet, S.; Jayakumar, H.; Dosa, P. I.; Feichtinger, K.; Casper, M.; Lehmann, J.; Jones, R. M.; Unett, D. J. Preparation of 3-phenylpyrazole derivatives as modulators of 5-HT2A serotonin receptors for the treatment of related disorders. WO2006055734, 2006.
    • Teegarden, B.; Xiong, Y.; Strah-Pleynet, S.; Jayakumar, H.; Dosa, P. I.; Feichtinger, K.; Casper, M.; Lehmann, J.; Jones, R. M.; Unett, D. J. Preparation of 3-phenylpyrazole derivatives as modulators of 5-HT2A serotonin receptors for the treatment of related disorders. WO2006055734, 2006.
  • 18
    • 68949158247 scopus 로고    scopus 로고
    • note
    • The solubilities of compound 13 (0.25 mg/ml in sodium phosphate buffer and 2.8 mg/ml in 0.01 N HCl) and compound 19 (0.15 mg/ml and 3.3 mg/ml) were similar to that of compound 3.
  • 20
    • 68949163580 scopus 로고    scopus 로고
    • note
    • Inhibition of the hERG channel varied based on the substituents in the compounds, but in general molecules containing the less basic morpholino group, like 54 and 56 (29% at 3 μM), showed less inhibition than those with more basic groups like 32 (90% at 3 μM) and 50 (64% at 1 μM).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.