sincalide and tetronothiodin

sincalide has been researched along with tetronothiodin* in 3 studies

Reviews

1 review(s) available for sincalide and tetronothiodin

Article	Year
[Cholecystokinin receptor antagonists]. Tanpakushitsu kakusan koso. Protein, nucleic acid, enzyme, 1993, Volume: 38, Issue:11 Topics: Amino Acid Sequence; Animals; Benzodiazepinones; Cholecystokinin; Furans; Indoles; Meglumine; Molecular Sequence Data; Proglumide; Receptors, Cholecystokinin; Sincalide; Thiophenes	1993

Other Studies

2 other study(ies) available for sincalide and tetronothiodin

Article	Year
Tetronothiodin, a novel cholecystokinin type-B receptor antagonist produced by Streptomyces sp. NR0489. II. Isolation, characterization and biological activities. The Journal of antibiotics, 1993, Volume: 46, Issue:1 A novel cholecystokinin type-B receptor antagonist named tetronothiodin has been isolated by column chromatography and preparative HPLC from the fermentation broth of Streptomyces sp. NR0489. Tetronothiodin inhibited the binding of CCK8 (C-terminal octapeptide of cholecystokinin) to rat cerebral cortex membranes (CCK type-B receptors) with an IC50 of 3.6 nM, whereas it did not inhibit CCK8 binding to rat pancreatic membranes (CCK type-A receptors). It also inhibited CCK8 induced Ca2+ mobilization in GH3 cells, a rat anterior pituitary cell line, but was without effect on the basal cytosolic Ca2+ concentration. This finding indicated tetronothiodin was an antagonist of CCK type-B receptors. Topics: Animals; Calcium; Cell Line; Cerebral Cortex; Chromatography, Gel; Chromatography, High Pressure Liquid; Furans; Magnetic Resonance Spectroscopy; Pancreas; Pituitary Gland, Anterior; Rats; Receptors, Cholecystokinin; Sincalide; Streptococcus; Thiophenes	1993
Tetronothiodin, a novel CCKB receptor ligand, antagonizes cholecystokinin-induced Ca2+ mobilization in a pituitary cell line. European journal of pharmacology, 1992, Oct-06, Volume: 221, Issue:1 We found a novel nonpeptide CCKB receptor antagonist, tetronothiodin (Ro 09-1468), in the culture broth of Streptomyces sp. NR0489. The structure of the compound (C31O8H38S), which has a 19-membered ring with an alpha-acyltetronic acid and tetrahydrothiophene moiety, is completely different from that of any known CCK receptor antagonist. Tetronothiodin inhibited [125I]CCK-8 binding to rat brain CCKB receptors with an IC50 of 3.6 nM, whereas it showed only weak affinity for rat CCKA receptors (IC50 = 70 microM). As demonstrated autoradiographically, tetronothiodin concentration dependently inhibited [125I]CCK-8 binding to CCKB receptors in rat forebrain slices. The effects of tetronothiodin on cytosolic Ca2+ concentrations in GH3 cells, a rat anterior pituitary tumor cell line, were investigated with the fura-2 method. Tetronothiodin inhibited CCK-8-induced Ca2+ mobilization without affecting basal cytosolic Ca2+ concentrations. In conclusion, tetronothiodin is a new, potent and highly selective CCKB receptor antagonist. It is a useful tool for investigating the pharmacological and physiological roles of CCKB receptors. Topics: Animals; Autoradiography; Binding Sites; Calcium; Cell Line; Cholecystokinin; Furans; Male; Pituitary Gland, Anterior; Rats; Rats, Wistar; Receptors, Cholecystokinin; Sincalide; Thiophenes	1992

Article

Year

Tetronothiodin, a novel cholecystokinin type-B receptor antagonist produced by Streptomyces sp. NR0489. II. Isolation, characterization and biological activities.

The Journal of antibiotics, 1993, Volume: 46, Issue:1

A novel cholecystokinin type-B receptor antagonist named tetronothiodin has been isolated by column chromatography and preparative HPLC from the fermentation broth of Streptomyces sp. NR0489. Tetronothiodin inhibited the binding of CCK8 (C-terminal octapeptide of cholecystokinin) to rat cerebral cortex membranes (CCK type-B receptors) with an IC50 of 3.6 nM, whereas it did not inhibit CCK8 binding to rat pancreatic membranes (CCK type-A receptors). It also inhibited CCK8 induced Ca2+ mobilization in GH3 cells, a rat anterior pituitary cell line, but was without effect on the basal cytosolic Ca2+ concentration. This finding indicated tetronothiodin was an antagonist of CCK type-B receptors.

Topics: Animals; Calcium; Cell Line; Cerebral Cortex; Chromatography, Gel; Chromatography, High Pressure Liquid; Furans; Magnetic Resonance Spectroscopy; Pancreas; Pituitary Gland, Anterior; Rats; Receptors, Cholecystokinin; Sincalide; Streptococcus; Thiophenes

1993

Tetronothiodin, a novel CCKB receptor ligand, antagonizes cholecystokinin-induced Ca2+ mobilization in a pituitary cell line.

European journal of pharmacology, 1992, Oct-06, Volume: 221, Issue:1

We found a novel nonpeptide CCKB receptor antagonist, tetronothiodin (Ro 09-1468), in the culture broth of Streptomyces sp. NR0489. The structure of the compound (C31O8H38S), which has a 19-membered ring with an alpha-acyltetronic acid and tetrahydrothiophene moiety, is completely different from that of any known CCK receptor antagonist. Tetronothiodin inhibited [125I]CCK-8 binding to rat brain CCKB receptors with an IC50 of 3.6 nM, whereas it showed only weak affinity for rat CCKA receptors (IC50 = 70 microM). As demonstrated autoradiographically, tetronothiodin concentration dependently inhibited [125I]CCK-8 binding to CCKB receptors in rat forebrain slices. The effects of tetronothiodin on cytosolic Ca2+ concentrations in GH3 cells, a rat anterior pituitary tumor cell line, were investigated with the fura-2 method. Tetronothiodin inhibited CCK-8-induced Ca2+ mobilization without affecting basal cytosolic Ca2+ concentrations. In conclusion, tetronothiodin is a new, potent and highly selective CCKB receptor antagonist. It is a useful tool for investigating the pharmacological and physiological roles of CCKB receptors.

Topics: Animals; Autoradiography; Binding Sites; Calcium; Cell Line; Cholecystokinin; Furans; Male; Pituitary Gland, Anterior; Rats; Rats, Wistar; Receptors, Cholecystokinin; Sincalide; Thiophenes

1992