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Volumn 17, Issue 3, 2007, Pages 657-661

Novel pyrazolopiperazinone- and pyrrolopiperazinone-based MCH-R1 antagonists

Author keywords

5HT 2C receptor; MCH R1 antagonists; Melanin concentrating hormone; Obesity; Pyrazolopiperazinone; Pyrrolopiperazinone

Indexed keywords

MELANIN CONCENTRATING HORMONE; MELANIN CONCENTRATING HORMONE ANTAGONIST; PYRAZOLE DERIVATIVE; PYRAZOLOPIPERAZINONE; PYRROLOPIPERAZINONE; UNCLASSIFIED DRUG;

EID: 33846231078     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.10.096     Document Type: Article
Times cited : (9)

References (26)
  • 1
    • 33846199885 scopus 로고    scopus 로고
    • note
    • The Surgeon General's Call to Action to Prevent and Decrease Overweight and Obesity 2001, Public Health Service: Office of the Surgeon General, US Department of Health and Human Sevices: Rockville, MD, 2001; www.surgeongeneral.gov/topics/obesity.
  • 16
    • 33846225969 scopus 로고    scopus 로고
    • Méndez-Andino, J. L.; Colson, A.-O.; Meyers, K. M.; Mitchell, M. C.; Hodge, K. M.; Howard, J. M.; Ackley, D. C.; Holbert, J. K.; Mittelstadt, S. W.; Dowty, M. E.; Obringer, C. M.; Suchanek, P; Reizes, O.; Hu, X. E.; Wos, J. A. Bioorg. Med. Chem., submitted for publication.
  • 17
    • 33846244566 scopus 로고    scopus 로고
    • Mieling, G. E.; Mieling, K. K.; Bush, R. D.; Colson, A.-O. US 2005170433 A1 2005.
  • 20
    • 33846207834 scopus 로고    scopus 로고
    • note
    • i) and maximal efficacy were determined and used to define structure-activity relationship.
  • 21
    • 33846240353 scopus 로고    scopus 로고
    • note
    • 3H] mesulergine and excess 10 μM mianserin (ICN). After incubating the mixture at room temperature for 60 min, bound mesulergine was separated from unbound mesulergine by filtration through glass fiber B filter (GF/B) plates (Millipore). Bound radioactive mesulergine was detected using a scintillation counter.
  • 23
    • 33846205956 scopus 로고    scopus 로고
    • Within our MCH program, we observed that compounds predicted to transport passively across the blood-brain barrier in the Caco-2 assay usually promoted statistically significant weight loss in our 4-day mDIO model, and displayed [brain]/[serum] > 2. Compounds predicted efflux substrates did not show in vivo activity and displayed [brain]/[serum] < 1.
  • 24
    • 33846255364 scopus 로고    scopus 로고
    • Please refer to: Meyers, K. M.; Méndez-Andino, J. L.; Colson, A. O.; Warshakoon, N. C.; Wos, J. A.; Mitchell, M. C.; Hodge, K. M.; Howard, J. M.; Ackley, D. C; Holbert, J. K.; Mittelstadt, S. W.; Dowty, M. E.; Obringer, C. M.; Ofer Reizes, O.; Hu, X. E. Bioorg. Med. Chem. Lett. 2006, 16, in press.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.