Pentagastrin meglumine

Names

[ CAS No. ]:
57448-84-7

[ Name ]:
Pentagastrin meglumine

Biological Activity

[Description]:

Pentagastrin (ICI-50123) meglumine is a potent, selective Cholecystokinin B (CCKB) receptor antagonists with IC50 values of 11 nM and 1100 nM for CCKB and CCKA, respectively. Pentagastrin meglumine enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury[1].[2].

[Related Catalog]:

Research Areas >> Cancer
Research Areas >> Endocrinology
Signaling Pathways >> GPCR/G Protein >> Cholecystokinin Receptor

[In Vitro]

Pentagastrin (ICI-50123) meglumine (0.1-100 μM; GH3-cells) increases intracellular Ca2+ in a dose-dependent manner with a maximal increase of 2.77-fold[1]. Pentagastrin (ICI-50123) meglumine (0.1-100 μM; GH3-cells) bounds dose dependently to GH3 cells[1].

[In Vivo]

Pentagastrin (ICI-50123) meglumine (80 µg/kg/h; i.v.; male Sprague-Dawley rats) protects rat gastric mucosa from acidified aspirin injury[2]. Animal Model: Male Sprague-Dawley rats[2] Dosage: 80 µg/kg/h Administration: Intravenous injection Result: Protected rat gastric mucosa from acidified aspirin injury. Induced a hyperaemic response to luminal acid challenge, increased mucus gel thickness, and elevated pHi during acid challenge.

[References]

[1]. Smith AJ, et al. Characterisation of CCKB receptors on GH3 pituitary cells: receptor activation is linked to Ca2+ mobilisation. Eur J Pharmacol. 1994 Apr 15;267(2):215-23.

[2]. Tanaka S, et al. Pentagastrin gastroprotection against acid is related to H2 receptor activation but not acid secretion. Gut. 1998 Sep;43(3):334-41.

Chemical & Physical Properties

[ Molecular Formula ]:
C44H66N8O14S

[ Molecular Weight ]:
963.11

Related Compounds