Chemistry and Pharmacology of SMS 201-995, a Long-Acting Octapeptide Analogue of Somatostatin

Pless, J.; Bauer, W.; Briner, U.; Doepfner, W.; Marbach, Peter; Maurer, Richard A.; Petcher, Trevor J.; Reubi, Jean–Claude; Vonderscher, Jacky

doi:10.3109/00365528609087432

Cited by 137 publications

(68 citation statements)

References 10 publications

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“…Oral administration indisputably offers therapeutic advantages, but its use is controversial, mainly because of the known enzymatic lability of peptides. Our interest was focused on the intestinal absorption of octreotide, which is stabilised against proteolytic degradation in GI fluids (Pless et al, 1986).…”

Section: Discussionmentioning

confidence: 99%

Enteral absorption of octreotide

Fricker

Drewe

Vonderscher

et al. 1992

British J Pharmacology

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1 The somatostatin octapeptide-analogue, octreotide, is absorbed as intact peptide from the gastrointestinal (GI) tract. 2 In situ absorption experiments in rats confirmed our recent intubation studies in human volunteers demonstrating that the peptide has preferential absorption sites in the small intestine. Absorption of octreotide was higher in the jejunum than in the duodenum or the ileum. 3 Experiments with bile-duct cannulated rats demonstrated that the absorption of octreotide decreased in the presence of bile, reflecting a negative influence of biliary components on the absorption of the peptide. 4 Uptake experiments using rat jejunal brush border membranes were performed to analyse the absorption mechanisms. The transport of octreotide into jejunal brush border membranes was significantly higher than the uptake into membrane vesicles isolated from rat ileum. When initial uptake (0-15 s) rates into the membrane vesicles were calculated as a function of the peptide concentration, a saturable component could be observed, indicative of transport mechanisms different from simple diffusion.

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Section: Discussionmentioning

confidence: 99%

Enteral absorption of octreotide

Fricker

Drewe

Vonderscher

et al. 1992

British J Pharmacology

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“…The somatostatin analogue octreotide has been in clinical use for treatment of NE tumours since the early 1980s. Somatostatin analogues are synthetic somatostatin octapeptide derivatives with structure and activities similar to those of the native hormone somatostatin, containing 14 amino acids, but with a significantly longer half-life and duration of action than the native substance (24).…”

Section: Therapymentioning

confidence: 99%

Guidelines for the management of gastroenteropancreatic neuroendocrine tumours (including bronchopulmonary and thymic neoplasms) Part I—General Overview

Öberg

Astrup²,

Eriksson³

et al. 2004

Acta Oncologica

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“…In the present study pertussis toxin alone had a small but significant effect on the basal intracellular levels of cyclic AMP but did not change the response to PGE2 (Figure 4b). As a control for the system we used SMS 201-995, a somatostatin analogue (Pless et al, 1986). Somatostatin induces multiple biological actions by interacting with a family of specific receptors, referred to as SSTRI-SSTR5 (Law et al, 1995), and all five receptors can be coupled to Gi, protein and inhibit adenylate cyclase (Viollet et al, 1995).…”

Section: Discussionmentioning

confidence: 99%

Characterization of the PGE₂ receptor subtype in bovine chondrocytes in culture

Brum‐Fernandes

Morisset

Bkaily

et al. 1996

British J Pharmacology

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1 Prostaglandin E2 (PGE2) is an autacoid that decreases proteoglycan synthesis, increases metalloprotease production by cultured chondrocytes, and can modulate some of the actions of interleukin-l on cartilage. The objective of the present study was to characterize the subtype of prostaglandin E2 receptor present in bovine chondrocytes in culture. 2 Primary cultures of articular chondrocytes were prepared from slices of bovine carpal cartilage by sequential digestion with type III hyaluronidase, trypsin, type II collagenase, followed by overnight incubation in Dulbecco's Modified Eagle's Medium (DMEM) with type II collagenase, washing, and seeding at a density of 2 x 105 cells cm-2 in DMEM with 10% foetal bovine serum.3 PGE2 and carbaprostacyclin induced dose-dependent increases in intracellular cyclic AMP in bovine chondrocytes in culture. The potencies of these compounds were different, and maximal doses of PGE2 and carbaprostacyclin had an additive effect. PGD2 induced a small increase in intracellular cyclic AMP only at a high concentration (10-' M).4 PGE2 was more potent that the EP2 agonist 11-deoxy-PGE, at inducing increases in intracellular cyclic AMP. The EP2 agonist butaprost, however, induced only a small increase at a concentration of l0-5 M. 17-Phenyl-PGE2 (EPI agonist), sulprostone and MB 28767 (15S-hydroxy-9-oxo-16-phenoxy-wotetranorprost-13E-enoic acid) (EP3 agonists) did not induce an increase in intracellular cyclic AMP at concentrations up to l0-' M. The EP4 antagonist AH 23848B ([1a(Z),2fl,5a]-(±)-7-[5-[[(l,1'-biphenyl)-4-yl]methoxy]-2-(4-morpholinyl)-3-oxocyclopentyl]-5-heptenoic acid) antagonized PGE2 but not carbaprostacyclin effects on intracellular cyclic AMP. The Schild plot slope was different from 1 but this could be due to an interaction of PGE2 with IP receptors in high doses. The exact nature of the antagonism by compound AH 23848B could not be definitely established in these experimental conditions. 6 Neither PGE2 nor any of its analogues inhibited the increase in intracellular cyclic AMP induced by forskolin, and pertussis toxin did not alter the response to PGE2, suggesting that no Gi-coupled PGE2 receptors are present in these cells. Stimulation with PGE2 did not induce significant increases in intracellular inositol-trisphosphate levels nor increases in intracellular free calcium as determined by confocal microscopy, suggesting the absence of phospholipase-C-coupled or of calcium channel-coupled PGE2 receptors in bovine chondrocytes in these experimental conditions. 7 These results show for the first time that bovine chondrocytes in culture present a functional PGE2 receptor that has some pharmacological characteristics of an EP4 subtype, as well as an IP receptor.

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Chemistry and Pharmacology of SMS 201-995, a Long-Acting Octapeptide Analogue of Somatostatin

Cited by 137 publications

References 10 publications

Enteral absorption of octreotide

Enteral absorption of octreotide

Guidelines for the management of gastroenteropancreatic neuroendocrine tumours (including bronchopulmonary and thymic neoplasms) Part I—General Overview

Characterization of the PGE₂ receptor subtype in bovine chondrocytes in culture

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Chemistry and Pharmacology of SMS 201-995, a Long-Acting Octapeptide Analogue of Somatostatin

Cited by 137 publications

References 10 publications

Enteral absorption of octreotide

Enteral absorption of octreotide

Guidelines for the management of gastroenteropancreatic neuroendocrine tumours (including bronchopulmonary and thymic neoplasms) Part I—General Overview

Characterization of the PGE2 receptor subtype in bovine chondrocytes in culture

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Characterization of the PGE₂ receptor subtype in bovine chondrocytes in culture