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.
James Black Foundation, 68 Half Moon Lane, Dulwich, London, SE24 9JE, UK. iain.mcdonald@kcl.ac.uk
Iain M
IM
McDonald
Carol
C
Austin
Ildiko M
IM
Buck
David J
DJ
Dunstone
Eric
E
Griffin
Elaine A
EA
Harper
Robert A D
RA
Hull
S Barret
SB
Kalindjian
Ian D
ID
Linney
Caroline M R
CM
Low
Michael J
MJ
Pether
John
J
Spencer
Paul T
PT
Wright
Trushar
T
Adatia
Alan
A
Bashall
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