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Paul J Gilligan

Explore the profile of Paul J Gilligan including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 24
Citations 99
Followers 0
Related Specialties
Chemistry
Biochemistry
Pharmacology
Top 10 Co-Authors
Ge Zhang
Robert Zaczek
Harvey Wong
Yu-Wen Li
George L Trainor
Snjezana Lelas
Argyrios G Arvanitis
John F McElroy
David W Robertson
Stephen P Arneric
Published In
Bioorg Med Chem Lett
J Med Chem
Psychopharmacology (Berl)
Curr Top Med Chem
J Pharmacol Exp Ther
Affiliations
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Recent Articles
11.
Dihydropyridopyrazinones and dihydropteridinones as corticotropin-releasing factor-1 receptor antagonists: structure-activity relationships and computational modeling
Dzierba C, Tebben A, Wilde R, Takvorian A, Rafalski M, Kasireddy-Polam P, et al.
J Med Chem . 2007 Apr; 50(9):2269-72. PMID: 17402721
The CRF antagonist pharmacophore is a heterocyclic ring bearing a critical hydrogen-bond acceptor nitrogen and an orthogonal aromatic ring. CRFR1 antagonists have shown a 40-fold and 200-fold loss in potency...
12.
Synthesis and evaluation of 2-anilino-3-phenylsulfonyl-6-methylpyridines as corticotropin-releasing factor1 receptor ligands
Hartz R, Arvanitis A, Arnold C, Rescinito J, Hung K, Zhang G, et al.
Bioorg Med Chem Lett . 2005 Nov; 16(4):934-7. PMID: 16297619
A novel series of 2-anilino-3-phenylsulfonyl-6-methylpyridines was synthesized and evaluated as corticotropin-releasing factor receptor ligands. Structure-activity relationship studies focused primarily on optimization of the 3-phenylsulfonyl group. Compounds within this series were...
13.
Effects of CRF1 receptor antagonists and benzodiazepines in the Morris water maze and delayed non-matching to position tests
Hogan J, Hodges Jr D, Lelas S, Gilligan P, McElroy J, Lindner M
Psychopharmacology (Berl) . 2005 Mar; 178(4):410-9. PMID: 15765256
Rationale: Benzodiazepines continue to be widely used for the treatment of anxiety, but it is well known that benzodiazepines have undesirable side effects, including sedation, ataxia, cognitive deficits and the...
14.
Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists
Dzierba C, Takvorian A, Rafalski M, Kasireddy-Polam P, Wong H, Molski T, et al.
J Med Chem . 2004 Oct; 47(23):5783-90. PMID: 15509177
Corticotropin releasing factor (CRF) is the primary regulator of the hypothalamus-pituitary-adrenal (HPA) axis, coordinating the endocrine, behavioral, and autonomic responses to stress. It has been postulated that small molecules that...
15.
Design, synthesis, and biological evaluation of 1,2,3,7-tetrahydro-6h-purin-6-one and 3,7-dihydro-1h-purine-2,6-dione derivatives as corticotropin-releasing factor(1) receptor antagonists
Hartz R, Nanda K, Ingalls C, Ahuja V, Molski T, Zhang G, et al.
J Med Chem . 2004 Sep; 47(19):4741-54. PMID: 15341489
A growing body of evidence suggests that CRF(1) receptor antagonism offers considerable therapeutic potential in the treatment of diseases resulting from elevated levels of CRF, such as anxiety and depression....
16.
Corticotropin-releasing factor antagonists: recent advances and exciting prospects for the treatment of human diseases
Gilligan P, Li Y
Curr Opin Drug Discov Devel . 2004 Sep; 7(4):487-97. PMID: 15338958
Corticotropin-releasing factor (CRF) co-ordinates the neural, endocrine and immune responses of the body to stress. Several studies have implicated CRF in the etiology of anxiety, depression, substance abuse, stress-related gastrointestinal...
17.
Anxiolytic-like effects of the corticotropin-releasing factor1 (CRF1) antagonist DMP904 [4-(3-pentylamino)-2,7-dimethyl-8-(2-methyl-4-methoxyphenyl)-pyrazolo-[1,5-a]-pyrimidine] administered acutely or chronically at doses occupying central CRF1...
Lelas S, Wong H, Li Y, Heman K, Ward K, Zeller K, et al.
J Pharmacol Exp Ther . 2004 Jan; 309(1):293-302. PMID: 14742750
Corticotropin-releasing factor(1) (CRF(1)) antagonists may be effective in the treatment of anxiety disorders with fewer side effects compared with classic benzodiazepines. The behavioral effects of DMP904 [4-(3-pentylamino)-2,7-dimethyl-8-(2-methyl-4-methoxyphenyl)-pyrazolo-[1,5-a]-pyrimidine] and its effects...
18.
Pyrazolo-[1,5-a]-1,3,5-triazine corticotropin-releasing factor (CRF) receptor ligands
Gilligan P, Folmer B, Hartz R, Koch S, Nanda K, Andreuski S, et al.
Bioorg Med Chem . 2003 Aug; 11(18):4093-102. PMID: 12927871
The syntheses and rat CRF receptor binding affinities of 'retro-pyrazolotriazine' corticotropin-releasing factor (CRF) ligands 4 are reported. Some have high affinity for rat CRF receptors (K(i)< or =10 nM). The...
19.
Pharmacological characterization of a novel nonpeptide antagonist radioligand, (+/-)-N-[2-methyl-4-methoxyphenyl]-1-(1-(methoxymethyl) propyl)-6-methyl-1H-1,2,3-triazolo[4,5-c]pyridin-4-amine ([3H]SN003) for corticotropin-releasing factor1 receptors
Zhang G, Huang N, Li Y, Qi X, Marshall A, Yan X, et al.
J Pharmacol Exp Ther . 2003 Mar; 305(1):57-69. PMID: 12649353
The in vitro pharmacological profile of a novel small molecule corticotropin-releasing factor 1 (CRF(1)) receptor antagonist, (+/-)-N-[2-methyl-4-methoxyphenyl]-1-(1-(methoxymethyl)propyl)-6-methyl-1H-1,2,3-triazolo[4,5-c]pyridin-4-amine (SN003), and the characteristics of its radioligand ([(3)H]SN003) are described. SN003 has high...
20.
CRF ligands via Suzuki and Negishi couplings of 3-pyridyl boronic acids or halides with 2-benzyloxy-4-chloro-3-nitropyridine
Arvanitis A, Arnold C, Fitzgerald L, Frietze W, Olson R, Gilligan P, et al.
Bioorg Med Chem Lett . 2002 Dec; 13(2):289-91. PMID: 12482442
A series of imidazo[4,5-b]pyridines with a 7-(3-pyridyl) substituent is described as high affinity CRF receptor ligands. Individual analogues were synthesized from key intermediates obtained via palladium-catalyzed coupling of 3-pyridyl zinc...