肾脏去神经会导致GLP-1不能增加肾小球滤过率,降低GLP-1的利钠和利尿作用[81],这也表明GLP-1的利钠利尿作用可能是由于抑制近端小管的钠重吸收,并强调GLP-1需要完整的肾神经支配来增加肾小球滤过。在啮齿动物和人的研究中表明GLP-1R在肾血管系统中表达[88]。GLP-1、exendin-4和DPP-4抑制剂西格列汀降低大鼠[...
Non-peptide compounds that act as antagonists of the intestinal hormone glucagon-like peptide 1 (GLP-1) have a 9H-尾-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent ...
GLP-1 A glucagon-like neuropeptide claimed to be an obesity mediator. Starved rats given the drug behave as if satiated and this state is reversed if given a GLP-1 antagonist. Collins Dictionary of Medicine © Robert M. Youngson 2004, 2005Want...
- Avexitide is a novel, first-in-class GLP-1 receptor antagonist with the potential to treat hyperinsulinemic hypoglycemia - FDA Breakthrough Therapy Designation granted for avexitide for post-bariatric hypoglycemia (PBH) and congenital...
GIPR antagonist antibodies conjugated to GLP-1 peptide are bispecific molecules that decrease weight in obese mice and monkeys. Cell Rep. Med. 2, 100263 (2021). PubMed PubMed Central Google Scholar Wang, Y. Z., Yang, D. H. & Wang, M. W. Signaling profiles in HEK 293T cells co-...
antagonist exendin-9 is centrally administered in rats [7] and when central GLP-1Rs are deleted in mice [8]. In this Review, we discuss similar preclinical studies that present novel concepts in the neural control of food intake and body weight, with reference to endogenous GLP-1, GLP-1R...
This conclusion is supported by the central finding of the present study that the highly selective GLP-1R antagonist Ex9 blocks the neuroprotective effect of RIC. Several studies reported the neuroprotective effects of GLP-1 and GLP-1R agonists in preclinical models of stroke [9, 21, 45]. Yet...
(Fig.1g–i). Greater insulin release with exendin-phe1 was unlikely to result from cross-reactivity with other incretin receptors, as it was blocked with the GLP-1R orthosteric antagonist exendin(9-39) (Supplementary Fig.2a). In accordance with its reduced capacity for stimulating insulin ...
It is interesting that only PKC-d translocation could be inhibited by the GLP-1R antagonist Ex9. In addition, brain infusion of Ex9 and calphostin C diabetes.diabetesjournals.org DIABETES 7 BRAIN GLP-1 SIGNALING, PKCs, AND BLOOD FLOW FIG. 6. Inhibition of brain GLP-1R signaling and ...
1 secretion.52 In humans, administration of atropine, a nonspecific mus- carinic-receptor antagonist, diminishes oral glucose-stim- ulated first-phase GLP-1 secretion independently of gas- tric emptying.53 In similar studies, either atropine or the M1 muscarinic-receptor antagonist pirenzepine could...