Novel, achiral 1,3,4-benzotriazepine analogues of 1,4-benzodiazepine-based CCK(2) antagonists that display high selectivity over CCK(1) receptors.
A series of 1,3,4-benzotriazepine-based CCK(2) antagonists have been devised by consideration of the structural features that govern CCK receptor affinity and the receptor subtype selectivity of 1,4-benzodiazepine-based CCK(2) antagonists. In contrast to the latter compounds, these novel 1,3,4-benzotriazepines are achiral, yet they display similar affinity for CCK(2) receptors to the earlier molecules and are highly selective over CCK(1) receptors.
McDonald
Iain M
IM
James Black Foundation, 68 Half Moon Lane, Dulwich, London, SE24 9JE, UK. iain.mcdonald@kcl.ac.uk
Austin
Carol
C
Buck
Ildiko M
IM
Dunstone
David J
DJ
Griffin
Eric
E
Harper
Elaine A
EA
Hull
Robert A D
RA
Kalindjian
S Barret
SB
Linney
Ian D
ID
Low
Caroline M R
CM
Pether
Michael J
MJ
Spencer
John
J
Wright
Paul T
PT
Adatia
Trushar
T
Bashall
Alan
A
D000818:Animals; D001552:Benzazepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001569:Benzodiazepines / Q000737:chemistry; D002460:Cell Line; D006224:Cricetinae; D003412:Cricetulus; D018360:Crystallography, X-Ray; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D011869:Radioligand Assay; D051381:Rats; D043886:Receptor, Cholecystokinin A / Q000037:antagonists & inhibitors* / Q000737:chemistry; D043887:Receptor, Cholecystokinin B / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D001552:Benzazepines; D043886:Receptor, Cholecystokinin A; D043887:Receptor, Cholecystokinin B; D001569:Benzodiazepines; C468549:Bz-423