Type A cholecystokinin receptor (CCKAR) antagonists differing in blood-brain barrier permeability were used to test the hypothesis that satiety is mediated, in part, by CCK action at CCKARs located peripheral to the blood-brain barrier. At dark onset, non-food-deprived rats received a bolus injection of devazepide (2.5 micromol/kg iv), a 3-h infusion of A-70104 (1 or 3 micromol x kg-1 x h-1 iv)...

This section, entitled "Pancreatic Pathology," includes a spectrum of topics on normal and abnormal pancreatic tissue. Specifically, two presentations deal with characterization of cholecystokinin (CCK) receptors on normal tissues. Wank has recently reported the purification, cloning, and expression of the CCKA receptor from rat pancreas, and the article by Miller deals with the biochemical cha...

To investigate GABA(B) receptors along vagal afferent pathways, we recorded from vagal afferents, medullary neurons, and vagal efferents in ferrets. Baclofen (7-14 micromol/kg i.v.) reduced gastric tension receptor and nucleus tractus solitarii neuronal responses to gastric distension but not gastroduodenal mucosal receptor responses to cholecystokinin (CCK). GABA(B) antagonists CGP-35348 or CG...

Type A cholecystokinin receptor (CCKAR) antagonists differing in blood-brain barrier permeability were used to test the hypothesis that duodenal delivery of protein, carbohydrate, and fat produces satiety in part by an essential CCK action at CCKARs located peripheral to the blood-brain barrier. Fasted rats with open gastric fistulas received devazepide (1 mg/kg iv) or A-70104 (700 nmol. kg(-1)...

The motility of the gut depends on the chemicals contained in the lumen, but the stimuli that modify motility and their relationship to enteric neural pathways are unclear. This study examined local inhibitory reflexes activated by various chemical stimulants applied to the mucosa to characterize effective physiological stimuli and the pathways they excite. Segments of the jejunum were dissecte...

1. The thalamic reticular nucleus (nRt) is innervated by cholecystokinin (CCK)-containing neurons and contains CCK binding sites. We used tight-seal, whole cell recording techniques with in vitro rat thalamic slices to investigate the action of CCK on neurons in nRt and ventrobasal thalamus (VB). 2. Brief applications of the CCK agonist cholecystokinin octapeptide (26-33) sulfated (CCK8S) evoke...

Submit Manuscript | http://medcraveonline.com Asperlicin was the first non-peptidal lead structure from nature [12] and analogues thereof were studied as CCK ligands [13]. Simplification of this lead structure by Merck led to Devazepide [14], a potent CCK1 selective cholecystokinin antagonist (Figure 1), containing a 1,4-benzodiazepine template and an indole moiety. Proglumide [15] was the firs...

Submit Manuscript | http://medcraveonline.com Asperlicin was the first non-peptidal lead structure from nature [12] and analogues thereof were studied as CCK ligands [13]. Simplification of this lead structure by Merck led to Devazepide [14], a potent CCK1 selective cholecystokinin antagonist (Figure 1), containing a 1,4-benzodiazepine template and an indole moiety. Proglumide [15] was the firs...