Pyrazolo-[1,5-a]-1,3,5-triazine corticotropin-releasing factor (CRF) receptor ligands.
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.
Gilligan
Paul J
PJ
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
Folmer
Beverly K
BK
Hartz
Richard A
RA
Koch
Stephanie
S
Nanda
Kausik K
KK
Andreuski
Stephen
S
Fitzgerald
Lawrence
L
Miller
Keith
K
Marshall
William J
WJ
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
D008024:Ligands; D011720:Pyrazoles; D018019:Receptors, Corticotropin-Releasing Hormone; D014227:Triazines; D003346:Corticotropin-Releasing Hormone