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Volumn 18, Issue 24, 2008, Pages 6423-6428

Identification of small molecule agonists of the motilin receptor

Author keywords

Agonist; GPCR; Motilin; Receptor

Indexed keywords

BIPHENYL DERIVATIVE; ERYTHROMYCIN; GASTROINTESTINAL AGENT; MEMBRANE RECEPTOR; MOTILIN; MOTILIN RECEPTOR; MOTILIN RECEPTOR AGONIST; UNCLASSIFIED DRUG;

EID: 56249141791     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.10.071     Document Type: Article
Times cited : (13)

References (22)
  • 14
    • 34250029161 scopus 로고    scopus 로고
    • Mccallum, R. W.; Cynshi, O. Aliment Pharmacol. Ther. 2007, 26(1), 107; See company websites: www.roche.com and www.pfizer.com.
    • Mccallum, R. W.; Cynshi, O. Aliment Pharmacol. Ther. 2007, 26(1), 107; See company websites: www.roche.com and www.pfizer.com.
  • 16
    • 56249123698 scopus 로고    scopus 로고
    • note
    • 2) was added. 10 μl from the compound plates was then added immediately to cell plates using a FLIPR 3 calcium imaging instrument and changes in fluorescence were measured over a 1 min timeframe. Maximum change in fluorescence over baseline was used to determine agonist response and concentration-response curves were constructed, using a 4-parameter logistic equation. The intrinsic activity of target compounds was calculated by using the maximum asymptote of its concentration-response curve relative to the maximum asymptote of the motilin concentration-response curve.
  • 18
    • 0344010043 scopus 로고    scopus 로고
    • It is unlikely that the activity observed for Compound 22 in the rabbit gastric antrum assay is partly or wholly due to action on the ghrelin receptor: other analogues in the series with no activity at the ghrelin receptor showed comparable or greater activity in the antrum assay (unpublished data); and ghrelin itself does not show enhancement of EFS mediated contractions in rabbit gastric antrum, see
    • It is unlikely that the activity observed for Compound 22 in the rabbit gastric antrum assay is partly or wholly due to action on the ghrelin receptor: other analogues in the series with no activity at the ghrelin receptor showed comparable or greater activity in the antrum assay (unpublished data); and ghrelin itself does not show enhancement of EFS mediated contractions in rabbit gastric antrum, see. Dass N.B., Hill J., Muir A., Testa T., Wise A., and Sanger G.J. Brit. J. Pharmacol. 140 (2003) 948
    • (2003) Brit. J. Pharmacol. , vol.140 , pp. 948
    • Dass, N.B.1    Hill, J.2    Muir, A.3    Testa, T.4    Wise, A.5    Sanger, G.J.6
  • 21
    • 56249099097 scopus 로고    scopus 로고
    • note
    • +).
  • 22
    • 56249132980 scopus 로고    scopus 로고
    • note
    • Westaway, S. M.; Brown, S. L.; Conway, E.; Heightman, T. D.; Johnson, C. N.; Lapsley, K.; Macdonald, G. J.; MacPherson, D. T.; Mitchell, D. J.; Myatt, J. W.; Seal, J. T.; Stanway, S. J.; Stemp, G.; Thompson, M.; Colombo, A.; Consonni, A.; Gagliardi, S.; Roccaboni, M.; Ronzoni, S.; Briggs, M. A.; Matthews, K. L.; Stevens, A. J.; Bolton, V. J.; Jarvie, E. M.; Stratton, S. C.; Sanger, G. J. Bioorg. Med. Chem. Lett. 2008, doi:10.1016/j.bmcl.2008.10.072.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.