Antibiotics & Metabolites

Activity: Macrolide antibiotic; Cytochrome P450 inhibitor . Function/Pharmacology: Macrolide antibiotic. Inhibits cytochrome P450 (IC50 = 0-5 µM), thus blocking CYP450-dependent drug oxidation.

Activity: Risperidone metabolite . Function/Pharmacology: Pharmacologically active metabolite of risperidone, an atypical antipsychotic agent.1 Displays high affinity for serotonin 5-HT2A receptors as well as dopamine D2 receptors.2,3 Chemical Name: 3-[2-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one

Activity: Quetiapine metabolite . Function/Pharmacology: Pharmacologically active metabolite of quetiapine.1 Exhibits distinct pharmacological activity from quetiapine and plays an important role in its antidepressant activity.2 Activates ERK1/2 and induces release of BDNF in C6 glioma cells which may contribute to the antidepressant properties of quetiapine.3 Inhibits the norepinephrine transporter which may contribute to the antipsychotic activity of quetiapine.4 Chemical Name: 11-(1-Piperazinyl)-dibenzo[b,f][1,4]thiazepine dihydrochloride

Activity: Fluoxetine metabolite . Function/Pharmacology: Metabolite of fluoxetine.3 Induces long QT syndrome via slow delayed rectifier potassium current block.1 Time dependent inhibitor of CYP2C19 and CYP3A4.2 The S-isomer of desmethylfluoxetine is the active N-demethylated metabolite responsible for the persistently potent and selective inhibition of serotonin uptake in vivo.3 Potent inhibitor of coxsackievirus replication acting via inhibition of viral RNA synthesis.4 State-dependent TREK-2 blocker.5 Chemical Name: 3-Phenyl-3-(4-trifluoromethyl-phenoxy)-propylamine hydrochloride (racemic)

Activity: Antibiotic . Function/Pharmacology: A cyclic anionic lipopeptide calcium-dependent antibiotic1. Useful for the treatment of serious Gram-positive infections including antibiotic-resistant strains such as MRSA and VRE2.

Activity: Antibiotic selection agent . Function/Pharmacology: A peptidyl nucleoside antibiotic inhibiting protein synthesis in bacteria and eukaryotes.1 Inhibits translation by trapping deformed tRNA on the ribosome.1 The ABC-type transporter NppA1A2BCD is required for uptake of blasticidin S and other peptidyl nucleoside antibiotics in Pseudomonas aeruginosa PA14.2 Selection agent for bis, bsr and bsd transformed cells.3,4 Chemical Name: (S)-4-[[3-Amino-5-[(aminoiminomethyl)methylamino]-1-oxopentyl]amino]-1-(4-amino-2-oxo-1(2H)-pyrimidinyl)-1,2,3,4-tetradeoxy-β-D-erythro-hex-2-enopyranuronic acid hydrochloride

Activity: Cytotoxic disulfide antibiotic . Function/Pharmacology: Displays potent broad-spectrum anticancer activity.1 Displays cytotoxic effects on mammalian cell lines (neuronal N2a cells and OLN-93 cells as model systems for nerve cells and glia) acting via disruption of mitochondrial membrane potential, activation of ERK1/2 and induction of HSP32/HO-1 (considered as a sensor of oxidative stress).2 A broad-spectrum antibiotic agent produced by marine bacteria which does not appear to induce resistance after long-term exposure.3 Chemical Name: Oxo-8,9-dithiabicyclo[5.2.0]non-1,4,6-triene-2-carboxylic acid

Activity: Antibiotic . Function/Pharmacology: Tigecycline is a clinically useful antibiotic.1,2 It is a glycylcycline derivative of minocycline that binds to the 30S ribosomal subunit of bacteria blocking the interaction of aminoacyl-tRNA with the ribosome. Tigecycline is active against Gram-positive and -negative bacteria, anaerobic bacteria and drug resistant bacteria such as MRSA, MRSE, and VRE. Tigecycline has also been shown to be selectively toxic to human acute myeloid leukemia cells over normal hematopoietic cells via inhibition of mitochondrial protein translation.3 It has also been found to be effective against other cancers including non-small cell lung cancer4, melanoma5, lymphoma6, and osteosarcoma7. Chemical Name: (4S,4aS,5aR,12aR)-9-[[2-(tert-Butylamino)acetyl]amino]-4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4H-tetracene-2-carboxamide

Activity: Cholesterol metabolite . Function/Pharmacology: Metabolite resulting from the action of sterol 27-hydroxylase on cholesterol. Concentrations of 27-hydroxycholesterol are elevated in patients with Alzheimers disease and mild cognitive impairment.1,2 Endogenous selective estrogen receptor modulator3 and ligand for the liver X receptor(EC50 = 85nM for LXRα and 71nM for LXRβ)4. Chemical Name: 27-Hydroxycholesterol; 5,25R-Cholesten-3β,26-diol