The ability of CCKA antagonists to inhibit full and partial CCK agonists of the rat pancreatic acinar cell CCKA receptor has been studied. When isolated rat pancreatic acini were superfused with CCK-8 (10 pM-1 nM) or CCK-4 (1 microM), an increase in [Ca2+]i signal was initiated. Concurrent superfusion of either L-364,718 (0.1 microM) or lorglumide (10 microM), chemically distinct, specific, pot...

We studied the effect of cholecystokinin (CCK) and the octapeptide of cholecystokinin (OP-CCK) on the feline gallbladder and sphinecter of Oddi. Both CCK caused a dose-dependent gallbladder contraction and sphincter of Oddi relaxation. The half-maximal responses of the sphincter of Oddi were 6 ng/kg for OP-CCK and 0.15 Ivy-dog U/kg for CCK, which were lower than those of the gallbladder with 28...

Panicogenic effects in humans of the selective cholecystokinin (CCK(B)) receptor agonist, cholecystokinin tetrapeptide (CCK4), have been reported to correlate with increases in heart rate (HR) and mean arterial pressure (MAP). Previous investigators have demonstrated that the nonselective CCK(A) and CCK(B) receptor agonist, sulfated cholecystokinin octapeptide, also produces increases in HR and...

Violation and discoordination of mental processes leads to changes in the ratio main neurotransmitters content further disorders. A significant role such is played by neuropeptides, particular anti-anxiety ones, which include cholecystokinin (CCK) its receptors. It has been established that stimulation CCK receptors modulates mesolimbic system reward, anxiety satiety. CCK-1 (the intestine) CCK-...

The effects of cholecystokinin (CCK) receptor antagonists on hypothermia induced by cocaine or morphine have been studied in mice. In the present work, subcutaneous (SC) injection of cocaine (50-150 mg/kg) or morphine (125-500 mg/kg) induced hypothermia in mice. Administration of CCKA receptor antagonist MK-329 (0.5-1.5 mg/kg), CCKB receptor antagonist L-365, 260 (0.5-1.5 mgl kg) and CCK r...

PD134308 and PD135158 are potent and selective antagonists at the cholecystokinin type B (CCK-B) receptors with IC50 values of 1.6 nM and 3.5 nM, respectively, in the radioligand binding assay and Ke values of 7.82 and 12.9 nM, respectively, in their blocking action on CCK responses in the rat lateral hypothalamic slice. PD134308 and PD135158 produced potent anxiolytic effects in the mouse blac...

Cholecystokinin (CCK) is an amino acid peptide. It has been isolated from porcine duodenum. CCK is known to regulate like anxiety, schizophrenia and depression by acting on CCKB receptor. CCK-A receptors are localized in the pancreas, gallbladder, pylorus, intestine and the vagus nerve. CCK is administered peripherally and it inhibits food consumption in humans and other many other species. CCK...

The control of cell proliferation by gastrin has been investigated in a rat pancreatic tumour cell line, AR4-2J. Exogenous gastrin, 10-12 to 10-8 M, stimulated cell growth of thymidine-synchronised AR4-2J cells cultured over 48 h in serum-free medium. Cell lysates of AR4-2J cells contained an average of 4.5 and 3.5 pg gastrin per 106 cells, when grown in serum-supplemented or serum-free media, ...

The gastric cholecystokinin-B/gastrin receptor (CCK-BR) is a key regulator of enterochromaffin-like cell function and proliferation. Over the last decade, a number of small non-peptide CCK-BR "antagonists" have been discovered. Here, we demonstrate that some of these non-peptide ligands in fact possess significant ability to activate the human CCK-BR, and are, therefore, more properly categoriz...