Literature DB >> 9171885

Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist.

Y L Chen1, R S Mansbach, S M Winter, E Brooks, J Collins, M L Corman, A R Dunaiskis, W S Faraci, R J Gallaschun, A Schmidt, D W Schulz.   

Abstract

The syntheses of a centrally active nonpeptide CRF1 receptor antagonist 2, butylethyl[2,5-dimethyl-7-(2,4,6-trimethylphenyl)-7H-pyrrolo [2,3-d]pyrimidin-4-yl]amine (CP-154,526), and its analogs 11-14 and [3H]-2 are reported. The in vitro CRF1 receptor binding affinity in the series 2, the pharmacokinetic properties of 2 in rats, and the anxiolytic-like effects of orally administered 2 are presented.

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Year:  1997        PMID： 9171885     DOI： 10.1021/jm960861b

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  12 in total

1.  Oral administration of a corticotropin-releasing hormone receptor antagonist significantly attenuates behavioral, neuroendocrine, and autonomic responses to stress in primates.

Authors:  K E Habib; K P Weld; K C Rice; J Pushkas; M Champoux; S Listwak; E L Webster; A J Atkinson; J Schulkin; C Contoreggi; G P Chrousos; S M McCann; S J Suomi; J D Higley; P W Gold
Journal:  Proc Natl Acad Sci U S A       Date:  2000-05-23       Impact factor: 11.205

2.  Corticotropin releasing factor-1 receptor antagonist, CP-154,526, blocks the expression of ethanol-induced behavioral sensitization in DBA/2J mice.

Authors:  J R Fee; D R Sparta; M J Picker; T E Thiele
Journal:  Neuroscience       Date:  2007-09-08       Impact factor: 3.590

Review 3.  Behavioral, biological, and chemical perspectives on targeting CRF(1) receptor antagonists to treat alcoholism.

Authors:  Eric P Zorrilla; Markus Heilig; Harriet de Wit; Yavin Shaham
Journal:  Drug Alcohol Depend       Date:  2013-01-05       Impact factor: 4.492

4.  Stress-induced behaviors require the corticotropin-releasing hormone (CRH) receptor, but not CRH.

Authors:  S C Weninger; A J Dunn; L J Muglia; P Dikkes; K A Miczek; A H Swiergiel; C W Berridge; J A Majzoub
Journal:  Proc Natl Acad Sci U S A       Date:  1999-07-06       Impact factor: 11.205

5.  Anxiogenic and aversive effects of corticotropin-releasing factor (CRF) in the bed nucleus of the stria terminalis in the rat: role of CRF receptor subtypes.

Authors:  Lacey L Sahuque; Erika F Kullberg; Andrew J Mcgeehan; Jennifer R Kinder; Megan P Hicks; Mary G Blanton; Patricia H Janak; M Foster Olive
Journal:  Psychopharmacology (Berl)       Date:  2006-03-28       Impact factor: 4.530

Review 6.  Progress in corticotropin-releasing factor-1 antagonist development.

Authors:  Eric P Zorrilla; George F Koob
Journal:  Drug Discov Today       Date:  2010-03-03       Impact factor: 7.851

7.  Urocortin, but not urocortin II, protects cultured hippocampal neurons from oxidative and excitotoxic cell death via corticotropin-releasing hormone receptor type I.

Authors:  Ward A Pedersen; Ruiqian Wan; Peisu Zhang; Mark P Mattson
Journal:  J Neurosci       Date:  2002-01-15       Impact factor: 6.167

8.  Blockade of the corticotropin releasing factor type 1 receptor attenuates elevated ethanol drinking associated with drinking in the dark procedures.

Authors:  Dennis R Sparta; Angela M Sparrow; Emily G Lowery; Jon R Fee; Darin J Knapp; Todd E Thiele
Journal:  Alcohol Clin Exp Res       Date:  2007-12-21       Impact factor: 3.455

9.  The role of corticotropin-releasing factor and corticosterone in stress- and cocaine-induced relapse to cocaine seeking in rats.

Authors:  S Erb; Y Shaham; J Stewart
Journal:  J Neurosci       Date:  1998-07-15       Impact factor: 6.167

10.  Allosteric modulators of class B G-protein-coupled receptors.

Authors:  Sam R J Hoare
Journal:  Curr Neuropharmacol       Date:  2007-09       Impact factor: 7.363
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