retention

Bethanechol chloride (Carbamyl-β-methylcholine chloride) is a slowly hydrolyzing muscarinic agonist with no nicotinic effects. It is used to increase smooth muscle tone in the GI tract following abdominal surgery or to treat urinary retention without obstruction. Possible side effects include hypotension, heart rate changes, and bronchial spasm.

Diammonium Glycyrrhizinate (Glycyrrhizin) , an extensively used anti-inflammatory agent, is isolated from the licorice root. It is metabolized to glycyrrhetinic acid, which inhibits 11-β-hydroxysteroid dehydrogenase and other enzymes involved in the metabolism of corticosteroids. Therefore, glycyrrhizic acid, the main and sweet component of licorice, has been studied for its ability to cause hypermineralocorticoidism with potassium loss and sodium retention, edema, increased blood pressure, as well as inhibited the renin-angiotensin-aldosterone system.

Prazosin hydrochloride (Vasoflex) reduces peripheral resistance and relaxes vascular smooth muscles as a selective adrenergic alpha-1 antagonist by a mechanism not completely known. Prazosin hydrochloride is a synthetic piperazine derivative with hypotensive antiadrenergic properties, It is used in the treatment of heart failure, hypertension, pheochromocytoma, Raynaud's syndrome, prostatic hypertrophy, and urinary retention.

DL-Mevalonolactone, a human endogenous metabolite, is the δ-lactone form of mevalonate, a precursor of the mevalonate pathway. It reduces mitochondrial membrane potential (∆Ψm), Ca2+ retention and NAD(P)H levels in the brain, and also induces mitochondrial swelling.DL-Mevalonolactone induces inflammation and oxidative stress, and reduces mitochondrial membrane potential.

Nadolol is a non-selective beta-adrenergic antagonist with antihypertensive and antiarrhythmic activities. Nadolol competitively blocks beta-1 adrenergic receptors located in the heart and vascular smooth muscle, inhibiting the activities of the catechola

Pinacidil (P 1134) is a guanidine that opens potassium channels and directly dilates peripheral blood vessels in small arteries, lowering blood pressure and peripheral resistance and producing fluid retention.

PK14105 has been evaluated biologically as a potential radioligand for positron emission tomography (PET) studies targeting peripheral benzodiazepine binding sites (PBBS) receptors. When administered to rats with unilaterally lesioned striata, PK14105 was observed to quickly cross the blood-brain barrier, displaying significant radioactivity retention in the lesioned striatum, in contrast to the unlesioned striatum or cerebellar vermis. Additionally, PK14105 has the capability to inhibit receptor ligands, calcium channel ligands, and co-transporters in all salivary glands.

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.

Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver, assisting BOS pharmacologically with 10%-20% activity retention.

Lu-AAZTA-NI-PSMA-093, a bivalent radiopharmaceutical agent designed for prostate cancer treatment, improves tumor targeting and retention. This is achieved by integrating a hypoxia-sensitive nitroimidazole (NI) group with a prostate-specific membrane antigen (PSMA) targeting moiety.

FAPI-mFS, an irreversible fibroblast activation protein (FAP) inhibitor, enhances uptake and retention in cancer cells through its covalent binding properties with FAP. When labeled with radioactive 68Ga or 177Lu, FAPI-mFS can be utilized for cancer imaging and therapy.

TDK-HCPT is a small molecule conjugate that links glutathione-sensitive thiamine disulfide with the chemotherapeutic agent 10-hydroxycamptothecin through a thioacetal bond. It targets tumor cells and prolongs the retention of the chemotherapeutic drug within these cells. TDK-HCPT inhibits tumor growth, induces apoptosis (apoptosis) in tumor cells, and exhibits antitumor activity.

DOTA-NI-FAPI-04 is an FAP inhibitor (IC50 = 7.44 nM). By integrating FAP targeting with hypoxia-sensitive groups (nitroimidazole), DOTA-NI-FAPI-04 significantly enhances tumor uptake and retention. Through DOTA chelation with metal isotopes (such as 68Ga and 177Lu), it forms radioactive probes ([68Ga]Ga DOTA-NI-FAPI-04 and [177Lu]Lu DOTA-NI-FAPI-04) useful for research in tumor diagnosis and therapeutics. This compound exhibits dual-targeting potential in cancer imaging, tumor microenvironment analysis, and radionuclide therapy, particularly in scenarios involving the interaction between tumor stroma and hypoxic regions.

Angiotensin I/II (2-7) is a peptide that contains the amino acids 2-7 and is converted from Angiotensin I/II peptide. Angiotensin is a peptide hormone that causes vasoconstriction and a subsequent increase in blood pressure. Angiotensin also stimulates th

Sdz 280 446 is one of the most active cyclopeptolide of many resistance-modifying agents in restoring rhodamine-123 retention within multidrug-resistant P388 cells.

CS-526 is a proton pump inhibitor. The inhibitory mechanism of CS-526 on H+,K+-ATPase was a competitive antagonism to the K+ binding site of H+,K+-ATPase, and it was also a reversible inhibition. CS-526 has a potent antisecretory effect on gastric acid se

Neostigmine Iodide is a parasympathic compound used as a reversible acetylcholinesterase inhibitor to improve muscle tone in patients with myasthenia gravis and in routine anesthesia to reverse the effects of non-depolarizing muscle relaxants such as rocu

Polythiazide (NSC-108161, P-2525) is used to treat fluid retention (edema) caused by a variety of causes, including congestive heart failure, severe liver disease (cirrhosis), kidney disease, or steroid or hormonal medication.

Sekdel sequence, as a signal, leads to retention of at least two proteins in the endoplasmic reticulum of animal cells.

(-)-L-threo-PDMP is an enhancer of ganglioside biosynthesis. The (-)-L-threo-PDMP (1S,2S) isomer is the active stimulatory component of DL-threo-PDMP in contrast to (+)-D-threo-PDMP , which is an inhibitor of glucosylceramide synthetase. (-)-L-threo-PDMP upregulates GM3, GD3, and GQ1b synthase levels, which are glycosyltransferases involved in ganglioside biosynthesis, and increases ganglioside levels in cells. It increases neurite outgrowth and synapse formation in vitro and improves retention of a long-term memory learned prior to forebrain ischemia in rats when administered following ischemia at a dose of 40 mg/kg per day.

8(R)-HETE is biosynthesized via lipoxygenation of arachidonic acid in marine invertebrates, including gorgonian corals and starfish. The stereochemical assignment of the (R) enantiomer is confirmed by comparing chiral HPLC retention times to published results.

8(S)-HETE, a major lipoxygenase product in PMA-treated murine epidermis, activates mouse keratinocyte protein kinase C with an IC50 of 100 μM and selectively activates PPARα at concentrations as low as 0.3 μM. The stereochemical assignment of the (S) enantiomer is based on comparison of chiral HPLC retention times to published results.

9(R)-HETE, which constitutes 50% of (±)9-HETE, activates RXRγ-dependent transcription 1.5-fold relative to a control at a concentration of 300 nM. The stereochemical assignment of the (R) enantiomer is based on the comparison of chiral HPLC retention times to published results.

9(S)-HETE is an enantiomer which makes up 50% of (±)9-HETE . There are no reports of 9(S)-HETE occurring as an enzymatic lipoxygenation product. Whereas 12(S)-HETE promotes adhesion of several cell lines to endothelial cell monolayes, 9(S)-HETE and other positional HETEs are without effect. Stereochemical assignment of the (S) enantiomer is based on comparison of chiral HPLC retention times to published results.