Fosinopril Sodium is the ester prodrug of an angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension and some types of chronic heart failure.Target: ACEFosinopril is a phosphinic acid-containing ester prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications. It is rapidly hydrolyzed to fosinoprilat, its principle active metabolite. Fosinoprilat inhibits ACE, the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Fosinopril may be used to treat mild to moderate hypertension, as an adjunct in the treatment of congestive heart failure, and to slow the rate of progression of renal disease in hypertensive individuals with diabetes mellitus and microalbuminuria or overt nephropathy [1-3].
Santacruzamate A is a potent and selective histone deacetylase inhibitor.
Sanguinarine chloride, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
Levoleucovorin calcium is the calcium salt of Levoleucovorin, which is the enantiomerically active form of folinic acid.IC50 value: Target: Levoleucovorin is used to treat or prevent toxic effects of methotrexate in people who have received methotrexate to treat bone cancer. Levoleucovorin is also used in combination chemotherapy with fluorouracil (5-FU) to treat colorectal cancer that has spread to other parts of the body. This medicine only treats the symptoms of colorectal cancer and does not treat the cancer itself.
Synephrine Hcl(Oxedrine) is an alkaloid; synephrine produces most of its biological effects by acting as an agonist at adrenergic receptors.IC50 value:Target: adrenergic receptor agonistThere is some evidence that synephrine also has weak activity at 5-HT receptors, and that it interacts with TAAR1 (trace adrenergic amine receptors). d-synephrine inhibited the uptake of [3H]-norepinephrine with an IC50 = 5.8 μM; l-synephrine was less potent (IC50 = 13.5 μM). d-Synephrine also competitively inhibited the binding of nisoxetine[m] to rat brain cortical slices, with a Ki = 4.5 μM; l-synephrine was less potent (Ki = 8.2 μM). In experiments on the release of [3H]-norepinephrine from rat brain cortical slices, however, the l-isomer of synephrine was a more potent enhancer of the release (EC50 = 8.2 μM) than the d-isomer (EC50 = 12.3 μM). This enhanced release by l-synephrine was blocked by nisoxetine.
Indaconitine is a natural product.
Danofloxacin Mesylate(CP76136-27 mesylate) is a fluoroquinolone antibacterial for veterinary use.Target: AntibacterialDanofloxacin is a synthetic antibacterial agent of the fluoroquinolone class, acts principally by the inhibition of bacterial DNA-gyrase, which is necessary for supercoiling of DNA to provide a suitable spatial arrangement of DNA within the bacterial cell. The minimum inhibitory concentration of danofloxacin against 90% (MIC90) of contemporary European and North American field isolates of Pasteurella haemolytica, Pasteurella multocida and Haemophilus somnus, the most important bacterial respiratory pathogens of cattle, is 0.125 μg/ml [1]. Danofloxacin shows protective dose (PD50) of 0.38, 0.8, 2.42 mg/kg for P. multocida, E. coli and S. choleraesuis in in vivo mouse protection assay [2].
Cantharidin, a natural toxin isolated from beetles in the families Meloidae and Oedemeridae, has been reported to be toxic to some pests, including the diamondback moth.IC50 value:Target:In vitro: A 48 h treatment of human erythrocytes with cantharidin significantly increased the percentage of annexin-V-binding cells (≥10 μg/mL), significantly decreased forward scatter (≥25 μg/mL), significantly increased [Ca2+]i (≥25 μg/mL), but did not significantly modify ceramide abundance or ROS [1]. In vivo:
Dictamnine (Dictamine) has the ability to exert cytotoxicity in human cervix, colon, and oral carcinoma cells; A natural plant product has been reported to have antimicrobial activity against bacteria and fungi.IC50 value:Target: Dictamnine has antimicrobial activities against the model fungus Saccharomyces cerevisiae, with a minimum inhibitory concentration (MIC) value of 64 microg/ml [1]. Dic induced S phase cell cycle arrest at low concentration and cell apoptosis at high concentration in which loss of mitochondrial membrane potential (Δψmm) was not involved. In addition, inhibition of caspase-3 using the specific inhibitor, z-DQMD-fmk, did not attenuate Dic-induced apoptosis, implying that Dic-induced caspase-3-independent apoptosis [2].
Halofuginone (RU-19110) is a less-toxic form of Febrifugine, which is isolated from the plant Dichroa febrifuga[1]. Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a Ki of 18.3 nM[2]. Halofuginone attenuates osteoarthritis (OA) by inhibition of TGF-β activity[3].
Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM.
Daurisoline is a hERG inhibitor and also an autophagy blocker.
Scopolamine hydrobromide is a high affinity (nM) muscarinic antagonist. 5-HT3 receptor-responses are reversibly inhibited by Scopolamine with an IC50 of 2.09 μM.
Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
5-Methyluridine is a is an endogenous methylated nucleoside found in human fluids.
Sinomenine hydrochloride is a blocker of the NF-κB activation and also an activator of μ-opioid receptor.
Ancitabine (hydrochloride) is an important antileukemia drugs.
Efavirenz is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture.
(-)-Sparteine is a natural alkaloid isolated from beans.
Fenspiride Hcl is an α adrenergic and H1 histamine receptor antagonist.IC50 value:Target: Adrenergic receptor; H1 receptorFenspiride hydrochloride is a bronchodilator with anti-inflammatory properties. Fenspiride hydrochloride inhibits mucus secretion and reduces the release of tachykinins at a prejunctional level. Fenspiride hydrochloride also may be an antagonist at α adrenergic and H1 histamine receptors.
Etimizol(Ethymisole; Antiffine; Ethylnorantifein) was shown to relieve amnesia effectively in the origin of which there is the hypoxic component (hypobaric hypoxia, actinomycin D, mechanical injury of the brain). IC50 Value: Target: Etimizol has a catalytic effect on the respiratory center and belongs to the group of respiratory analeptics, however, it activates adrenokortikotropnuyu pituitary function, which leads to increased levels of glucocorticosteroids in the blood. There is also evidence that short etimizol improves memory and increases mental performance.in vitro:in vivo: The time interval between administration ofetimizol (3 mg/kg) and the onset of learning varied between 0.5 and 3 h in the several series. Etimizol did not facilitate the learning in rats whatever the time of administration and biological modality of reinforcement [1]. After administration of etimizol at doses of 10 or 1 mg/loop mean residence time of etimizol in the loop was 20.1 and 7.6 min, respectively, with mean standard deviation being 3.1 and 0.8, respectively [2]. Extracellular application of 5--10 mM/L etimizol exerted a specific effect on the giant neurons of the Coretus corneus isolated nervous system: action potential duration increased significantly, speed of development of its descending phase decreased, as well as the trace hyperpolarization amplitude [3].
Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins.Target: Alpha-1A adrenergic receptorNicergoline acts by inhibiting the postsynaptic alpha(1)-adrenoceptors on vascular smooth muscle. This inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation. Nicergoline displaced [3H]-prazosin bound to rat forebrain membranes pretreated with chloroethylclonidine (pKi = 9.9 +/- 0.2) at concentrations 60-fold lower than in rat liver membranes (pKi = 8.1 +/- 0.2). Finally, of the nicergoline metabolites studied, lumilysergol acted as a modest alpha 1 antagonist (bromonicotinic acid was devoid of alpha 1 antagonist activity). In conclusion, nicergoline is a potent and selective alpha 1A-adrenoceptor subtype antagonist, an alpha 1-adrenoceptor subtype which is mainly represented in resistance arteries [1].
Aconine inhibits receptor activator of nuclear factor (NF)-κB ligand (RANKL)-induced NF-κB activation.
Oxaceprol is an anti-inflammatory drug used in the treatment of osteoarthritis. Oxaceprol markedly inhibited inflammatory cell infiltration and bone damage in the adjuvant-injected paw. oxaceprol was effective at inhibiting periarticular soft tissue inflammation.[1] IV Injection: 50mg/kg.[2]
Lycorine (hydrochloride) is VE-cadherin inhibitor,and has IC50 of 1.2μM in Hey1B cell.IC50: 1.2μM (Hey1B cell)[2]In vitro:Lycorine (hydrochloride) executed an anti-melanoma vasculogenic effect by inhibiting VE-cadherin gene expression in C8161 cells and caused a decrease in cell surface exposure of VE-cadherin protein. Consistently, LH significantly suppressed VE-cadherin gene promoter activity. [1]Lycorine (hydrochloride) effectively inhibited mitotic proliferation of Hey1B cells (half maximal inhibitory concentration = 1.2 μM) with very low toxicity, resulting in cell cycle arrest at the G2/M transition through enhanced expression of the cell cycle inhibitor p21 and marked down-regulation of cyclin D3 expression. Moreover, LH suppressed both the formation of capillary-like tubes by Hey1B cells cultured in vitro.[2]In vivo: Lycorine effectively suppressed C8161 cell-dominant tumor formation and generation of tumor blood vessels in vivo with low toxicity.[1]Lycorine (hydrochloride) suppressed the formation of the ovarian cancer cell-dominant neovascularization in vivo when administered to Hey1B-xenotransplanted mice, suggest that LH selectively inhibits ovarian cancer cell proliferation and neovascularization and is a potential drug candidate for anti-ovarian cancer therapy.[2]
Moxifloxacin is a synthetic fluoroquinolone antibiotic agent.Target: AntibacterialMoxifloxacin is an extended-spectrum fluoroquinolone which has improved coverage against gram-positive cocci and atypical pathogens compared with older fluoroquinolone agents, while retaining good activity against gram-negative bacteria. The antibacterial spectrum of moxifloxacin includes all major upper and lower respiratory tract pathogens; it is one of the most active fluoroquinolones against pneumococci, including penicillin- and macrolide-resistant strains [1]. Moxifloxacin has limited phototoxic potential. In clinical trials, moxifloxacin had clinical success rates of 88-97% and bacteriologic eradication rates of 90-97%. Moxifloxacin is a safe and effective antimicrobial that will be useful for treating acute sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia [2]. Moxifloxacin possibly stimulates lipid peroxidation and enhances phagocytosis, as depicted by MDA production and survival prolongation, without being toxic as depicted by white blood cell count [3]. Clinical indications: Abdominal abscess; Acute bronchitis; Acute sinusitis; Bacterial infectionToxicity: Symptoms of overdose include CNS and gastrointestinal effects such as decreased activity, somnolence, tremor, convulsions, vomiting, and diarrhea. The minimal lethal intravenous dose in mice and rats is 100 mg/kg.
Wilforine is a sesquiterpene pyridine alkaloid; importantbioactive compound in T. wilfordii plants, and is effective intreating idiopathic pulmonary fibrosis.
Tandospirone citrate is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM). IC50 Value: 27±5 nM(Ki) [1]Target: 5-HT1Ain vitro: Tandospirone is most potent at the 5-HT1A receptor, displaying a Ki value of 27 +/- 5 nM. The agent is approximately two to three orders of magnitude less potent at 5-HT2, 5-HT1C, alpha 1-adrenergic, alpha 2-adrenergic, and dopamine D1 and D2 receptors (Ki values ranging from 1300 to 41000 nM). Tandospirone is essentially inactive at 5-HT1B receptors; 5-HT uptake sites; beta-adrenergic, muscarinic cholinergic, and benzodiazepine receptors [1]. 3H-SM-3997 bound rapidly, reversibly and in a saturable manner with high affinity to rat brain hippocampal membranes (Kd = 9.4 nM, Bmax = 213 fmol/mg protein) [2]. in vivo: Chronic treatment with tandospirone, at 0.2 and 1.0mg/kg/day, but not 2.0mg/kg/day, attenuated footshock stress-induced eLAC elevation in the mPFC [3]. Rats were acutely administered tandospirone (0, 0.1, and 1 mg/kg, i.p.). Tandospirone decreased the number of premature responses, an index of impulsive action, in a dose-dependent manner [4].Toxicity: It is not believed to be addictive but it is known to produce mild withdrawal effects (e.g. anorexia) after abrupt discontinuation.
Atropine sulfate is a competitive muscarinic acetylcholine receptor antagonist.IC50 value:Target: mAChRAtropine is a naturally occurring tropane alkaloid extracted from deadly nightshade (Atropa belladonna), Jimson weed (Datura stramonium), mandrake (Mandragora officinarum) and other plants of the family Solanaceae. Atropine is a competitive antagonist of the muscarinic acetylcholine receptors (acetylcholine being the main neurotransmitter used by the parasympathetic nervous system). Atropine dilates the pupils, increases heart rate, and reduces salivation and other secretions [1].
ATP is a phosphate-group donor for substrate activation in metabolic reactions and the coenzyme for a large number of kinases.