4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2, 4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: a potent, orally bioavailable CRF(1) receptor antagonist.

@article{He2000413Dimethoxyprop2ylamino27dimethyl824A,
  title={4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2, 4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: a potent, orally bioavailable CRF(1) receptor antagonist.},
  author={Liqi He and Paul J. Gilligan and Robert C. Zaczek and Lawrence W. Fitzgerald and John McElroy and Helen Shen and J A Saye and Ned H. Kalin and S J Shelton and Daryl Christ and George L. Trainor and Peter Hartig},
  journal={Journal of medicinal chemistry},
  year={2000},
  volume={43 3},
  pages={
          449-56
        }
}
Structure-activity studies in the pyrazolo[1,5-a]-1,3,5-triazine series led to the discovery that compound 11i (DMP696) is a potent hCRF(1) receptor antagonist (K(i) = 1.7 nM vs 7.5 nM for alpha-hel-CRF(9-41), hCRF(1) adenylate cyclase IC(50) = 82 nM vs 286 nM for alpha-hel-CRF(9-41)). Compound 11i has excellent oral pharmacokinetic profiles in rats and dogs (37% and 50% oral bioavailabilities, respectively). This compound displays good activity in the rat situational anxiety model (MED = 3 mg… CONTINUE READING
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American journal of physiology. Regulatory, integrative and comparative physiology • 2001
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