intestinal secretion

Lidamidine (Lidamidinum) is an effective antidiarrheal agent that inhibits intestinal secretion, reduces intestinal transit, and inhibits smooth muscle contraction.

Celiprolol hydrochloride (Selectrol) is a cardioselective beta-1 adrenergic antagonist that has intrinsic sympathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION.

Glp-1(7-37) acetate is an intestinal insulin hormone that enhances glucose-induced insulin secretion.

GLP-1(7-36) Acetate is a major intestinal hormone that stimulates glucose-induced insulin secretion from β cells.

Neuropeptide Y (NPY), a neuropeptide, plays roles in regulating appetite, vasoconstriction, cardiac contractility, and intestinal secretion, acting as an agonist for NPY receptors Y1, Y2, and Y5. Expressed ubiquitously, NPY modulates cellular responses by selectively inhibiting forskolin-induced cAMP accumulation in L-M(TK-) cells expressing rat Y1 or Y2 and in HEK293 cells expressing rat Y5, more so than in cells expressing rat Y4 receptors (EC50s = 0.15, 2.7, 0.66, and >1,000 nM, respectively). Additionally, it elevates perfusion pressure in isolated guinea pig hearts (EC30 = 1.3 nM) and, when administered intracerebroventricularly at 300 pmol/animal, it notably increases food intake in rats.

PACAP (1-38), a novel neuropeptide isolated from the bovine hypothalamus is more active than vasoactive intestinal peptide (VIP) in stimulating adenylate cyclase (EC50=7 nM). PACAP 1-38 (10-9 M) increased substance P (SP), gastrin releasing peptide (GRP),

Lidamidine Hydrochloride is an alpha2-adrenergic receptor agonist. Lidamidine Hydrochloride inhibits intestinal secretion, reduces intestinal transit, and inhibits smooth muscle contraction.

Lubiprostone (hemiketal) (RU-0211 (hemiketal)), a selective activator of the chloride channel 2 (CLCN2), facilitates the treatment of chronic idiopathic constipation and opioid-induced constipation. It functions by enhancing CLCN2 channel activity, which boosts chloride ion secretion in the intestines, subsequently increasing fluid secretion and improving intestinal peristalsis. Additionally, Lubiprostone (hemiketal) may be utilized in research related to chronic constipation and cancer.

GLP-1(7-36), amide TFA is a prominent intestinal hormone that stimulates glucose-induced insulin secretion from β cells[1].

CP-66948 is a potent histamine H2 receptor antagonist with inhibitory effect on gastric acid secretion and can be used to protect gastric and intestinal mucosa.

Gastric inhibitory peptide (GIP) (1-42), an endogenous incretin hormone comprising 42 amino acids, promotes insulin secretion. Expressed in the intestinal neuroendocrine K cells and submandibular gland, it enters circulation after meals. GIP (1-42) blocks histamine, pentagastrin, and insulin-induced gastric acid and pepsin secretion, enhances glucose-stimulated insulin release, and accelerates gastric emptying in rats.

MK-8666 is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects.

BMS-986118 is a full agonist of GPR40, is a G-protein-coupled receptor expressed primarily in pancreatic islets and intestinal L-cells that has been a target of significant recent therapeutic interest for type II diabetes. Activation of GPR40 by partial a

PACAP (1-38) free acid TFA, an endogenous neuropeptide, effectively enhances antral motility and somatostatin secretion, while concurrently suppressing gastrin secretion and promoting the release of vasoactive intestinal polypeptide, gastrin-releasing peptide, and substance P. Additionally, it amplifies N-methyl-D-aspartate receptor function and brain-derived neurotrophic factor expression via RACK1 [1] [2].

PACAP (1-38) free acid, an endogenous neuropeptide, potently modulates gastrointestinal and neuroendocrine functions. It enhances antral motility, increases somatostatin secretion, and stimulates the release of vasoactive intestinal polypeptide, gastrin releasing peptide, and substance P, while concurrently inhibiting gastrin secretion. Additionally, it augments N-methyl-D-aspartate receptor function and upregulates brain-derived neurotrophic factor expression via RACK1 [1] [2].

GIP, human TFA, a 42-amino acid peptide hormone, functions as a glucose-dependent insulin secretion stimulator and a weak gastric acid secretion inhibitor. Released from intestinal K cells following nutrient ingestion, it serves as an incretin hormone [1] [2] [3].

Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear leukocytes (PMN) with IC50 values of 29 and 14 µM, respectively. Flufenamic acid also activates various ion channels, including transient receptor potential canonical 6 (TRPC6) and the large-conductance calcium-activated potassium channel (KCa1.1). It also inhibits various ion channels, including TRPC3 and the cystic fibrosis transmembrane conductance regulator (CFTR). Flufenamic acid (20 mg/kg) reduces increases in intestinal fluid secretion and intestinal barrier disruption in mice ......

Neuropeptide Y (NPY) (3-36) is a C-terminal fragment of NPY, a neuropeptide involved in controlling appetite, blood pressure, cardiac contractility, and intestinal secretion. NPY (3-36) is an endogenous peptide produced by cleavage of NPY by dipeptidyl peptidase 4 (DPP-4). It binds selectively to the NPY receptor Y2 (Ki = 0.41 nM in CHP 234 cells) over the Y1 receptor, where it does not bind at concentrations up to 1 μM. NPY (3-36) (0.1 nM) increases migration of human umbilical vein endothelial cells (HUVECs) by 80% after 12 hours in an in vitro wound closure assay. NPY (3-36) corresponds to residues 3-36 of the human and rat protein sequence.

Zolimidine, an imidazopyridine derivative, functions as an orally active antiulcer agent. It promotes mucus secretion in intestinal mucosal cells and enhances the intestinal wall's resistance to ulceration. Studies demonstrate its gastroprotective effect in duodenal ulcer research [1] [2].

GLP-1 receptor agonist. Endogenous preproglucagon-derived neuropeptide that modulates feeding and metabolism. Also secreted by intestinal L-cells. Increases cAMP production and inhibits gastric acid secretion in rat stomach. Also weak glucagon receptor ag

MK-8666 Tris is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 Tris has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects.

BAA473, a bile acid analog, is a potent activator of the pyrin inflammasome, inducing secretion of interleukin-18 (IL-18) through inflammasome activation in both myeloid and intestinal epithelial cells [1].

Flufenamic acid (Arlef) is an anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth and topically.