title: Pyrazolo-[1,5-a]-1,3,5-triazine corticotropin-releasing factor (CRF) receptor ligands.
abstract: 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 data provide additional support for the hypothesis that it is possible to interchange isosteric cores with similar electronic properties in the design of high-affinity CRF receptor ligands, provided the peripheral pharmacophore elements are maintained in the same three-dimensional array.
authors.affiliation: Bristol-Myers Squibb Co., Discovery Chemistry Department and E.I. DuPont de Nemours and Co., Central Research and Development Department, Experimental Station, Wilmington, DE 19880-0500, USA. paul.j.gilligan@bms.squibb
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Gilligan
authors.forename: Beverly K
authors.initials: BK
authors.lastname: Folmer
authors.forename: Richard A
authors.initials: RA
authors.lastname: Hartz
authors.forename: Stephanie
authors.initials: S
authors.lastname: Koch
authors.forename: Kausik K
authors.initials: KK
authors.lastname: Nanda
authors.forename: Stephen
authors.initials: S
authors.lastname: Andreuski
authors.forename: Lawrence
authors.initials: L
authors.lastname: Fitzgerald
authors.forename: Keith
authors.initials: K
authors.lastname: Miller
authors.forename: William J
authors.initials: WJ
authors.lastname: Marshall
mesh_terms: D000818:Animals; D001665:Binding Sites; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D003346:Corticotropin-Releasing Hormone / Q000737:chemistry / Q000494:pharmacology; D066298:In Vitro Techniques; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D011720:Pyrazoles / Q000737:chemistry*; D051381:Rats; D018019:Receptors, Corticotropin-Releasing Hormone / Q000145:classification / Q000187:drug effects*; D014227:Triazines / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D008024:Ligands; D011720:Pyrazoles; D018019:Receptors, Corticotropin-Releasing Hormone; D014227:Triazines; D003346:Corticotropin-Releasing Hormone