GLP-1 receptor: difference between revisions
Diff·revision 13 → 14·04:16, 17 Dec 2024
Difference between revision 13 and revision 14 of GLP-1 receptor. 2 lines changed; the page grew by 335 bytes.
| Revision 13 — 22:43, 21 Nov 2024 SatietySunniva (talk) convert the receptor-distribution list to a table 5,187 bytes +119 | Revision 14 — 04:16, 17 Dec 2024 LabRangeLindy (talk) the glucose-dependence of the insulinotropic effect deserves its own sentence 5,522 bytes +335 | ||
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| 35 | Bias has been proposed as a design lever: an agonist that produces sustained cAMP with reduced β-arrestin recruitment internalises the receptor less, maintains surface expression, and might therefore sustain insulin secretion better over prolonged exposure. Evidence for this in humans is indirect, and the ''in vitro'' bias factors reported for marketed agonists have not been shown to predict clinical differences.{{r|jones2018}} | 35 | Bias has been proposed as a design lever: an agonist that produces sustained cAMP with reduced β-arrestin recruitment internalises the receptor less, maintains surface expression, and might therefore sustain insulin secretion better over prolonged exposure. Evidence for this in humans is indirect, and the ''in vitro'' bias factors reported for marketed agonists have not been shown to predict clinical differences.{{r|jones2018}} |
| 36 | 36 | ||
| + | 37 | Desensitisation ''in vivo'' is limited. Tachyphylaxis to the insulinotropic effect is not observed clinically at therapeutic exposures, whereas tachyphylaxis to the gastric-emptying effect is well documented and is one reason the delay in emptying attenuates over months of treatment while glycaemic effect persists.{{r|drucker2018}} | |
| + | 38 | ||
| 37 | == References == | 39 | == References == |
| 38 | {{reflist}} | 40 | {{reflist}} |