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Mediation by CCKB receptors of the CCK‐evoked hyperaemia in rat gastric mucosa
1 Cholecystokinin octapeptide (CCK‐8) and gastrin‐17 augment gastric mucosal blood flow in the rat. The present study examined whether the gastric vasodilator effect of these peptides is mediated byExpand
Alanine scan and N-methyl amide derivatives of Ac-bombesin[7-14]. Development of a proposed binding conformation at the neuromedin B (NMB) and gastrin releasing peptide (GRP) receptors.
Alanine and N-methylation scans together with molecular modelling were implemented in order to propose a binding conformation of the minimum active fragment of bombesin (BB), Ac-BB[7-14], to theExpand
'Targeted' molecular diversity: design and development of non-peptide antagonists for cholecystokinin and tachykinin receptors.
A drug design strategy to non-peptide small molecule antagonists of neuropeptides is described that targets the molecular diversity which exists in the 'privileged' data set of the physico-chemicalExpand
A Trp in chi space
Our aim is to identify and synthesise a ‘family’ of tryptophan mimetics which thoroughly explore chi space and then incorporate them into selected ligands for biological receptors e.g. TachykininExpand
Peptide-Like Drugs May be Excluded from the Brain by P-Glycoprotein at the Blood-Brain Barrier
Peptide-like compounds, particularly a NK1 antagonist and to a small extent CCKA and CCKB antagonists, appear to interact with P-glycoprotein since they show effects on intracellular drugExpand
A Trp in chi space
Our aim is to identify and synthesise a ‘family’ of tryptophan mimetics which thoroughly explore chi space and then incorporate them into selected ligands for biological receptors e.g. TachykininExpand