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

Natalizumab is a recombinant humanized monoclonal antibody and a humanized monoclonal antibody inhibitor that selectively targets α4 integrin (CD49d). Natalizumab binds to the α4β1 heterodimer and blocks its interaction with vascular cell adhesion molecule 1. Natalizumab also prevents lymphocytes from entering the central nervous system, thereby preventing acute demyelinating relapses, and is used in the study of relapsing-remitting multiple sclerosis and Crohn’s disease. Natalizumab possesses anti-inflammatory and immunomodulatory activity, inhibiting the adhesion, retention, and transendothelial migration of immune cells, and reducing the infiltration of inflammatory cells into the central nervous system or affected sites. Natalizumab is also being studied for autoimmune or inflammation-related diseases such as B-cell lymphoma and non-infectious uveitis.

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.

(R)-(-)-α-Methylhistamine dihydrobromide is a potent, selective, and brain-penetrant agonist of the H3 histamine receptor with high receptor affinity, capable of enhancing memory retention and attenuating cognitive impairment in rat models, making it a valuable pharmacological probe for elucidating central histaminergic signaling and H3 receptor-mediated modulation of learning and memory processes.

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.

AB-3PRGD2 is a radiolabeled agent that targets integrin αvβ3. It enhances tumor uptake and prolongs retention time in tumors, significantly improving the inhibition of tumor growth. AB-3PRGD2 also remodels the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8+ T cells.

DOTAGA-FAP-2286-ALB is a derivative of Rofapitide tetraxetan. It functions as a selective inhibitor of fibroblast activation protein (FAP) with an IC50 value of 67.5 nM. By interacting with albumin, DOTAGA-FAP-2286-ALB enhances tumor retention, prolongs circulation time in the bloodstream, and improves the stability of radiometal complexes [such as 111In and 225Ac]. This compound shows promise for use in targeted radionuclide therapy (TRT) research for FAP-positive solid tumors.

C105SR is a cyclophilin D (CypD) inhibitor targeting peptidyl-prolyl cis-trans isomerase (PPIase). It has an IC50 value of 5 nM for inhibiting mitochondrial permeability transition pore (mPTP) opening. C105SR reduces apoptosis in hepatocytes induced by hypoxia-reoxygenation and boosts calcium retention capacity (CRC). It demonstrates hepatoprotective effects in a mouse model of ischemia-reperfusion injury (IRI).

ETN029 is a ligand targeting DLL3. The 225Ac-labeled ETN029 exhibits dose-dependent cytotoxic effects on small cell lung cancer (SCLC), neuroendocrine prostate cancer (NEPC), and metastatic melanoma cells, and can induce H2AX phosphorylation. The 177Lu-labeled ETN029 has rapid tumor uptake, sustained retention, and a favorable tumor-to-renal distribution ratio. Therefore, ETN029 can be used for imaging and mechanism studies of tumors such as SCLC and NEPC.

BWD is a PSMA ligand (IC50 = 35.86) known for its excellent in vitro stability and high affinity. It enhances tumor uptake and retention, inhibits tumor growth in vivo, and is applicable in cancer research.

DOTA-ALB-01 is an albumin-binding FAP inhibitor (FAPI) ligand. When labeled with 68Ga or 177Lu, DOTA-ALB-01 exhibits high FAP binding affinity and enhances tumor uptake and retention. DOTA-ALB-01 is utilized in PET/CT and SPECT/CT imaging for cancer, particularly in advanced stages.

DOTA-ALB-02 is a ligand that binds with albumin and acts as an FAP inhibitor (FAPI). When labeled with 177Lu, DOTA-ALB-02 demonstrates high affinity for FAP, enhancing tumor uptake and retention, and it has a significant tumor-to-nontarget ratio. It is used in PET/CT and SPECT/CT imaging for detecting cancer, particularly advanced stages.

FAP-IN-7 (Compound 5b) is a FAP inhibitor. The 18F-labeled version of FAP-IN-7 improves tumor retention and demonstrates high selectivity along with favorable pharmacokinetics. It can serve as a radioactive tracer for cancer PET imaging and radionuclide therapy research.

Betamethasonesuccinate (NSSL-BMS) is a nanoformulation capable of crossing the blood-brain barrier, created by encapsulating Betamethasone hemisuccinate in PEGylated liposomes. By leveraging the enhanced permeability and retention effect of liposomes, Betamethasone succinate effectively delivers potent glucocorticoids to inflammatory sites. It inhibits the secretion of pro-inflammatory cytokines, such as TNF-α and IL-6, while maintaining the levels of the anti-inflammatory cytokine TGF-β. This compound is useful for researching arthritis and cerebral malaria.