reabsorption

Lotrifen (Privaprol), an agent of non-hormonal antifertility, causes the arrest and involution of pregnancy. It acts, after the implantation of the blastocyst, directly on the product of conception, which undergoes a slow and gradual degenerative process and ends with the reabsorption or expulsion of it.

Trichlormethiazide (Naqua) is a short-acting, 3-dichloromethyl derivative of hydrochlorothiazide, belonging to the class of thiazide diuretics. Trichlormethiazide appears to block the active reabsorption of chloride and possibly sodium in the ascending loop of Henle, altering electrolyte transfer in the proximal tubule.

Atomoxetine hydrochloride (LY 139603) is the hydrochloride salt of atomoxetine, a phenoxy-3-propylamine derivative and selective non-stimulant, norepinephrine reuptake inhibitor with cognitive-enhancing activity. Although its precise mechanism of action is unknown, atomoxetine appears to selectively inhibit the pre-synaptic norepinephrine transporter, resulting in inhibition of the presynaptic reabsorption of norepinephrine and prolongation of norepinephrine activity in the synaptic cleft. The effect on cognitive brain function may result in improved attention and decreased impulsivity and activity levels.

Dapagliflozin (BMS-512148) is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.

Mildronate (Meldonium) is an inhibitor of biosynthesis of L-carnitine by gamma-butyrobetaine (GBB) hydroxylase and as a competitive inhibitor of renal carnitine reabsorption.

Dapagliflozin ((2S)-1,2-propanediol, hydrate) (BMS-512148 (2S)-1,2-propanediol, hydrate) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2), in development for treating type 2 diabetes mellitus (T2DM). It inhibits SGLT2, responsible for at least 90% of glucose reabsorption in the kidney.

Mildronate dihydrate is an inhibitor of biosynthesis of L-carnitine by gamma-butyrobetaine (GBB) hydroxylase and as a competitive inhibitor of renal carnitine reabsorption.

Lesinurad (RDEA594) is a selective inhibitor of uric acid reabsorption which is used in combination with other agents in the therapy of gout. Lesinurad has had a limited clinical use but has not been associated with serum enzyme elevations during therapy or with instances of clinically apparent liver injury.

Desmopressin acetate (16679-58-6 free base) (DDAVP) is the synthetic analog of the antidiuretic hormone arginine vasopressin. Vasopressin Receptor The antidiuretic properties of desmopressin have led to its use in polyuric conditions including primary nocturnal enuresis, nocturia, and diabetes insipidus. Desmopressin acetate (16679-58-6 free base) works by limiting the amount of water that is eliminated in the urine. Desmopressin acetate (16679-58-6 free base) binds to V2 receptors in renal collecting ducts, increasing water reabsorption. It also stimulates the release of von Willebrand factor from endothelial cells by acting on the V2 receptor.

Disulfamide is an orally active carbonic anhydrase inhibitor with an IC50 value of 0.07 μM. Disulfamide has a diuretic effect by inhibiting carbonic anhydrase and preventing the reabsorption of sodium and bicarbonate in the proximal convoluted tubules.

1. Desoxyrhaponticin (Deoxyrhaponticin) is an agent that is potentially effective in controlling postprandial hyperglycemia in diabetes, the in vivo antidiabetic action of this compound can be explained, in part at least, by inhibition of glucose transport in the small intestine and inhibition of glucose reabsorption in the kidney. 2. Desoxyrhaponticin and rhaponticin could be considered as promising fatty acid synthase(FAS) inhibitors, they could inhibit intracellular FAS activity and downregulate FAS expression in human breast cancer MCF-7 cells.

Amiloride hydrochloride dihydrate (Amiloride HCl dihydrate) is a pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride hydrochloride dihydrate is used in conjunction with DIURETICS to spare POTASSIUM loss.

Benzthiazide (Lemazide) is used in the therapy of edema and hypertension. Like other thiazides, benzthiazide accelerates water loss from the body (diuretics). They inhibit Na+ Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.

Dotinurad ((3,5-dichloro-4-hydroxyphenyl)(1,1-dioxidobenzo[d]thiazol-3(2H)-yl)methanone) is a potent agent of uricosuric (IC50: 3.6 μM for uric acid).

Fludrocortisone acetate (9α-Fludrocortisone acetate), a glucocorticoid-receptor agonist, binds to cytoplasmic receptors, translocates to the nucleus, and initiates transcription of glucocorticoid-responsive genes like lipocortins to inhibit phospholipase A2 (PLA2). As the acetate salt of a synthetic fluorinated corticosteroid, it exhibits anti-inflammatory and antiallergic activities. PLA2 inhibition prevents arachidonic acid release, a precursor of eicosanoids such as prostaglandins and leukotrienes, which are key mediators in the pro-inflammatory response. As a mineralocorticoid-receptor agonist, it stimulates Na+ reabsorption, water retention, and K+ and H+ secretion in the distal tubules and collecting ducts of the kidney.

Canagliflozin hemihydrate (TA 7284) is a drug of the gliflozin class or subtype 2 sodium-glucose transport inhibitors used for the treatment of type 2 diabetes. SGLT2 is responsible for at least 90% of renal glucose reabsorption (SGLT1 being responsible for the remaining 10%). Blocking this transporter causes up to 119 grams of blood glucose per day to be eliminated through the urine, corresponding to 476 kilocalories.

Lesinurad sodium (RDEA594 sodium) is a selective inhibitor of uric acid reabsorption and is used in the study of cardiovascular diseases.

AA 193 selectively inhibits the presecretory reabsorption of uric acid.

Colesevelam Hydrochloride is a bile acid sequestrant with a higher affinity for glycocholic acid in vitro. Colesevelam Hydrochloride inhibits bile acid reabsorption, leading to increased bile acid synthesis and reduces cholesterol levels in patients with

Chlorthalidone impurity G is a potential impurity found in commercial preparations of chlorthalidone that has moderate antihypertensive effects. Chlorthalidone is a thiazide-like diuretic that inhibits the Na+/Cl- cotransporter in the distal convoluted tubule of the kidney, which prevents reabsorption of sodium and chloride leading to a reduction in plasma volume and cardiac output. It also inhibits carbonic anhydrase (CA), including the isoforms CAVB, VII, IX, XII, and XIII (Kis = 2.8-23 nM) and, to a lesser extent, CAI, CAII, IV, VA, and VI (Kis = 138-1,347 nM), which may mediate its sustained vasodilatory activity. Dietary administration of chlorthalidone (8 mg per animal per day) reduces arterial hypertension and prevents or reduces ventricular hypertrophy induced by deoxycorticosterone acetate (DOCA) in salt-hypertensive rats. Formulations containing chlorthalidone have been used alone or in combination with other antihypertensive agents to lower arterial blood pressure and as adjuvants to address edema caused by cardiac or renal disorders.

Desmopressin (DDAVP)(DDAVP) is the synthetic analogue of the antidiuretic hormone arginine vasopressin.Vasopressin Receptor The antidiuretic properties of desmopressin have led to its use in polyuric conditions including primary nocturnal enuresis, nocturia, and diabetes insipidus. Desmopressin works by limiting the amount of water that is eliminated in the urine. Desmopressin binds to V2 receptors in renal collecting ducts, increasing water reabsorption. It also stimulates release of von Willebrand factor from endothelial cells by acting on the V2 receptor.

Puliginurad (YL-90148) is a potent and selective inhibitor of the urate transporter protein (URAT), effectively inhibiting uric acid reabsorption. It can be utilized for the prevention and treatment of hyperuricemia and gout.

Prorenoate is a steroidal aldosterone antagonist with potassium-sparing diuretic activity. Prorenoate antagonizes the activity of aldosterone at the mineralocorticoid receptor in the nephron and thereby prevents sodium reabsorption. This interferes with the sodium potassium exchanger and causes sodium and water excretion while reducing potassium excretion.

YM-543, also known as ASP-543, is a selective SGLT2 inhibitor. Sodium-glucose cotransporter 2 (SGLT2) is a specifically expressed transporter in the kidney that plays an important role in renal glucose reabsorption, and its inhibition may present a novel therapeutic strategy for treating diabetes. YM543 potently and selectively inhibited mouse and human SGLT2 activities at nanomolar ranges. In vivo single oral administration of YM543 dose-dependently and significantly reduced blood glucose levels and improved glucose tolerance with a concomitant increase in urinary glucose excretion in KK Ay type 2 diabetic mice, effects that were sustained even after 12 h.