Activators & Inhibitors

Activity: Antioxidant-phenolic . Function/Pharmacology: Potent antioxidant. Cell permeable. Chemical Name: 4,4’-Methylenebis(2,6-di-tert-butylphenol)

Activity: TRPV1 agonist . Function/Pharmacology: Capsaicin is a vanilloid agonist known to activate the transient receptor potential channel vanilloid subfamily member 1 (TRPV1)1,2 and to possess analgesic3, anti-inflammatory4 and hypolocomotor effects5. SEVERE IRRITANT - HANDLE WITH CARE Chemical Name: 8-Methyl-N-vanillyl-trans-6-nonenamide

Activity: Spin trap . Function/Pharmacology: Hydrophilic spin trap for superoxide, O-, C-, S- and N-centered free radicals. Useful for both in vivo and in vitro studies. Cell Permeable. Chemical Name: 5,5-Dimethyl-1-pyrroline N-oxide

Activity: Antifibrotic . Function/Pharmacology: Antifibrotic agent. Prevents lung fibrosis in bleomycin-induced animal models.1 Down-regulates bleomycin-induced overexpression of lung procollagen I and III genes.2 Up-regulates RGS2 (Regulator of G-protein Signaling 2) which represents a new mechanism of pirfenidone action.3 Inhibits fibroblast proliferation.4 Suppresses TNFα production at the translational level.5 Scavenges hydroxyl radicals and inhibits lipid peroxidation in a dose-dependent manner.6 Recently approved therapeutic agent for idiopathic pulmonary fibrosis.7 Orally active. Chemical Name: 5-Methyl-1-phenyl-2(1H)-pyridinone

Activity: Dopamine D2 agonist . Function/Pharmacology: A semi-synthetic ergoline derivative which acts as a partial dopamine D2 agonist and 5HT2B/2C receptor antagonist. Displays antiparkinsonian effects in MPTP-treated cynomolgus monkeys1. Partial agonist at recruitment of -arrestin2 to the D2 receptor2. Ameliorates monocrotaline-induced pulmonary hypertension in rats3. Chemical Name: S(+)-N,N-Diethyl-N′([8α]-6-methylergolin-8-yl)urea

Activity: Microtubule depolymerizing agent . Function/Pharmacology: A naturally occurring alkaloid which acts as an antimitotic agent by binding to tubulin and depolymerizing microtubules. Induces apoptosis in a variety of cell lines. Chemical Name: (S)-N-(5,6,7,9-Tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo[a]heptalen-7-yl)acetamide

Activity: Dopamine receptor partial agonist . Function/Pharmacology: Clinically useful neuroleptic and antipsychotic agent1. Dopamine D2 receptor antagonist and autoreceptor agonist2. Improves symptoms of psychosis associated with Alzheimer’s disease3. Blocks cocaine-seeking behavior without affecting other rewarding behaviors in animal models4. Chemical Name: 7-[4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydro-2(1H)-quinolinone

Activity: MAO-B inhibitor, Neuroprotective . Function/Pharmacology: Potent, irreversible monoamine oxidase (MAO) inhibitor selective for MAO-B (IC50=4.43 nM) over MAO-A (IC50=412 nM).1 Parkinson’s disease therapeutic.2 Displays neuroprotective and neurorestorative properties in a Parkinson’s disease zebrafish model.3 Prevents -synuclein-induced dopaminergic neuronal death and rescues TrkB neurotrophic signaling.4 Enhances BDNF levels and is neuroprotective in Parkinson’s disease models.5 Chemical Name: (1R)-2,3-Dihydro-N-2-propynyl-1H-inden-1-amine methanesulfonate

Activity: Induces remyelination of neurons . Function/Pharmacology: Centrally acting M1 muscarinic acetylcholine receptor antagonist (Ki=0.59 nM, rat).1 Also inhibits the dopamine transporter (Ki=160 nM).2 Enhances remyelination and significantly decreases clinical severity in the experimental autoimmune encephalomyelitis model of relapsing-remitting multiple sclerosis alone or in combination with immunosuppressive agents.3 Inhibits hepatitis C virus infection.4 Chemical Name: 3-(Endo)-3-(diphenylmethoxy)-8-methyl-8-azabicyclo[3.2.1]octane methanesulfonate