ArticleBritish journal of pharmacology2007
A functional comparison of recombinant and native somatostatin sst2 receptor variants in epithelia.
Article in British journal of pharmacology, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
5 citing papers in PubMed, 12 citations in OpenAlex.
- International Union of Basic and Clinical Pharmacology. CV. Somatostatin Receptors: Structure, Function, Ligands, and New Nomenclature.Pharmacological reviews · 2018Review
- Activation of submucosal 5-HT(3) receptors elicits a somatostatin-dependent inhibition of ion secretion in rat colon.British journal of pharmacology · 2010Article
- Site specificity of agonist and second messenger-activated kinases for somatostatin receptor subtype 2A (Sst2A) phosphorylation.Molecular pharmacology · 2009Article
- Selective agonism in somatostatin receptor signaling and regulation.Molecular and cellular endocrinology · 2008Review
- Endothelin-converting enzyme-1 degrades internalized somatostatin-14.Endocrinology · 2008Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeSomatostatin (SRIF-14) exerts broad spectrum antisecretory effects by activating the somatostatin 2 (sst(2)) receptor. The rat (r) sst(2) receptor exists in 'long' (sst(2a)) and 'short' (sst(2b)) forms that differ in their C termini, while a single human (h) sst(2a) exists. This study compares the characteristics of recombinant rsst(2a), rsst(2b) and hsst(2a) activation in human epithelia, and with native sst(2) responses in rat colon. EXPERIMENTAL APPROACH: Epithelial layers of each clone or rat colon were placed in Ussing chambers and short-circuit current (I (SC)) measured in response to SRIF-14 and chosen analogues. The relative potencies and ability to cause desensitization to SRIF-14 were assessed, and the affinities of the sst(2) antagonist, D-Tyr(8) CYN154806 for hsst(2a), rsst(2a) and native rat colon sst(2) receptors were established. KEY
resultsBasolateral SRIF-14 responses were transient in hsst(2a) and rsst(2a) epithelia, but prolonged in rsst(2b)-expressing cells. Activation of rsst(2a) resulted in significant desensitization to SRIF-14 and receptor phosphorylation, whereas the rsst(2b) receptor did neither. Sst(2)-preferred agonists (BIM23190C and BIM23027) reduced I (sc) with similar potency and both caused complete desensitization to SRIF-14. CYN154806 antagonized hsst(2a) and rsst(2a) receptors with pK (B) values of 7.9 and 7.8, respectively. In rat colon mucosa, CYN154806 blocked SRIF-14 responses with a pA (2) value of 8.2, and BIM23190C responses with a pK (B) of 8.4. CONCLUSIONS AND IMPLICATIONS: SRIF-14 caused rapid rsst(2a) receptor phosphorylation and desensitization of epithelial antisecretory responses, neither of which occurred with the rsst(2b) receptor. These mechanisms are most likely to be a prerequisite for sensitivity to sst(2)-analogues with radiotherapeutic potential.
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