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A potent, orally bioavailable benzazepinone growth hormone secretagogue

Academic Article
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Overview

authors

  • DeVita, R. J.
  • Bochis, R.
  • Frontier, A. J.
  • Kotliar, A.
  • Fisher, M. H.
  • Schoen, W. R.
  • Wyvratt, M. J.
  • Cheng, K.
  • Chan, W. W. S.
  • Butler, B.
  • Jacks, T. M.
  • Hickey, G. J.
  • Schleim, K. D.
  • Leung, K.
  • Chen, Z. S.
  • Chiu, S. H. L.
  • Feeney, W. P.
  • Cunningham, P. K.
  • Smith, Roy

publication date

  • May 1998

journal

  • Journal of Medicinal Chemistry  Journal

abstract

  • The identification of L-739,943 (8b), a potent, orally bioavailable benzolactam growth hormone secretagogue, is obtained from zwitterionic L-692,429 through modification of its amino acid side chain and replacement of the acidic 2'-tetrazole with the neutral and potency enhancing 2'-(N-methylaminocarbonylamino)methyl substituent. L-739,943 is orally active for the release of growth hormone in beagle dogs at doses as low as 0.5 mg/kg. Oral bioavailability in dogs of 8b is 24% at a dose of 2 mg/kg with a mean drug Cmax of 145 +/- 46 ng/mL. L-739,943 represents a significant breakthrough in terms of both potency and oral bioavailability as compared to the prototype benzolactam L-692,429.

subject areas

  • Administration, Oral
  • Animals
  • Benzazepines
  • Biological Availability
  • Cells, Cultured
  • Dogs
  • Female
  • Growth Hormone
  • Male
  • Methylurea Compounds
  • Pituitary Gland
  • Rats
  • Rats, Wistar
  • Structure-Activity Relationship
  • Tetrazoles
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Identity

International Standard Serial Number (ISSN)

  • 0022-2623

Digital Object Identifier (DOI)

  • 10.1021/jm970816j

PubMed ID

  • 9572898
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Additional Document Info

start page

  • 1716

end page

  • 1728

volume

  • 41

issue

  • 10

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