Pargyline is an irreversible inhibitor of monoamine oxidase (MAO) that is used clinically to treat moderate hypertension. At 10 mg/kg iv, pargyline induces a moderate decrease of systolic blood pressure in unanaesthetized hypertensive rats but not normotensive WKR or Sprague-Daley rats. The…

An orally active broad spectrum antifungal agent that blocks ergosterol biosynthesis by inhibiting the fungal CYP isoform CYP51; potently inhibits the mammalian analog CYP51A1 (IC₅₀ = 63.5 nM), as well as a variety of other CYP isoforms.

An NSAID commonly used in animals to combat pain and inflammation, particularly as associated with osteoarthritis; inhibits both COX-1 and COX-2 (IC₅₀s = 22.3 and 3.9 µM, respectively) and also FAAH (IC₅₀ = 74 µM).

Capsaicin is the primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper. Capsaicin is present in natural hot pepper extracts along with a number of impurities, including dihydrocapsaicin and several lesser impurities. Separation by HPLC is required in…

A prodrug for A-771726 that regulates T lymphocyte progression through the cell cycle by selectively inhibiting de novo pyrimidine synthesis; used to slow the disease progression of rheumatoid arthritis and as an immunosuppressive agent to prevent rejection of transplant allografts and xenografts.

A dihydropyridine L-type calcium channel blocker that selectively inhibits calcium influx in cardiac and vascular smooth muscle; inhibits calcium-induced contractions in depolarized rat aorta (IC₅₀ = 1.9 nM), displaying a slow rate of association and dissociation in isolated vascular and…

A cell-permeable, stable free radical that is commonly used to evaluate the ability of compounds to act as free radical scavengers or hydrogen donors and to measure the antioxidant activity of tissue extracts; followed by color change from purple (absorbance at 515-528 nm) to yellow.

A DNA alkylating agents that induces DNA interstrand and intrastrand crosslinks, cytotoxicity, and apoptosis; inhibits the growth of PC-3 prostate cancer cells with IC₅₀ values of 0.074 or 0.77 μM for sequential dosing or single dosing, respectively.

The primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper and present in natural hot pepper extracts; elicits a sensation of burning pain by activation of TRPV1 on small, non-myelinated polymodal C-type nociceptive nerve fibers and has been widely…

An amino-amide anesthetic that binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, preventing the generation of an action potential; inhibits the uptake of dopamine in striatal synaptosomes by 47% at 100 µM.

A thio analog of the purine base guanine that incorporates into DNA during replication, inducing double-strand breaks that destabilize its structure and result in cytotoxicity; used as a chemotherapeutic for acute leukemia and other types of cancer, including BRCA2-mutated tumors.

An agonist of muscarinic receptors (EC₅₀ = 1.8-17 µM for human M2).

A histamine H1 receptor antagonist (Ki = 9 nM) that is effective against HCV (EC₅₀ = 44 nM), preventing viral entry into host cells.

An immunomodulatory and antiproliferative compound that interacts directly with the protein CRBN (IC₅₀ = 8.5 nM), a ubiquitously-expressed E3 ligase, and DDB1 complexes.

A potent antagonist of dopamine receptors (IC₅₀s = 1.0 and 0.9 nM for D2 and D3, respectively);,also avidly binds α1- and α2-adrenergic receptors, histamine H1 receptor, and serotonin (5-HT) receptors 5-HT1D and 5-HT2A (Kis = 10, 80, 3.4, 19, 1.2 nM, respectively).

An anti-protozoal agent; prevents misfolding of prion protein (EC₅₀ = 0.3 μM), blocks voltage-dependent sodium channels (IC₅₀ = 3.3 μM), inhibits aldehyde oxidase (IC₅₀ = 3.3 μM), antagonizes the riboflavin-binding protein (Ki = 6.7 μM), inhibits…

An irreversible inhibitor of AChE (IC₅₀ = 4.15 µM) and BuChE (IC₅₀ = 37 nM); used in modifying the course of neurodegenerative diseases.

A phenothiazine classified as an antipsychotic compound; antagonizes dopamine and serotonin receptors (Kis = 0.66, 0.84, 1.2, and 1.8 nM for D2, D3, D4, and 5-HT2A, respectively); also antagonizes histamine, α1- and α2-adrenergic, and muscarinic acetylcholine receptors.

An α2-adrenergic receptor agonist (Kd = 7.6 nM for rat cerebral cortex membranes) that has transient antihypertensive effects; used in managing opioid withdrawal symptoms during detoxification from heroin and methadone.

A centrally acting α2-adrenergic receptor agonist that decreases peripheral vascular resistance by centrally inhibiting sympathetic nerve activity; also acts as an agonist of the imidazoline (I1) receptor (Ki = 4-8 nM).

An inhibitor of URAT1 (IC₅₀ = 0.3 µM for hURAT1) that prevents renal urate resorption; also potently inhibits CYP2C9 (Ki = 20 nM) and has been used to study adverse drug-drug interactions.

Blocks and reverses platelet aggregation induced by such triggers as collagen, U-46619, and ADP (IC₅₀ = 1.1, 2.1, and 4.1 µM, respectively); reduces tyrosine phosphorylation in stimulated platelets and inhibits recombinant human Syk and Src (IC₅₀ = 2.8 and 27.3 µM,…

A non-selective inhibitor of NOS isoforms in vitro (IC₅₀s = 0.71, 0.78, and 5.8 µM for rat nNOS, bovine eNOS, and rat iNOS, respectively); shows good anti-nociceptive effects without affecting blood pressure via inhibition of eNOS in vivo.

An NSAID that potently inhibits both COX-1 and COX-2 (IC₅₀s = 5 and 8 nM, respectively); used, in a variety of different formulations, as an analgesic.

An inhibitor of CTP:phosphocholine cytidylyl transferase with antimetastatic properties.

A butyrophenone derivative which is used in the treatment of schizophrenia and delirium; binds to the dopamine D2 receptor (Ki = 0.1 nM), antagonizing dopamine signaling.

A natural naphthoquinone that has allelopathic actions, suppressing growth, photosynthesis, and respiration in plants and other organisms; irreversibly inhibits peptidyl-prolyl cis/trans isomerases of the parvulin family, including human Pin1, yeast Ess1/Ptf1, and E. coli parvulin (Ki = 55.9 nM).

A gold-thiol complex with anti-inflammatory and immunosuppressive actions; potently inhibits thioredoxin reductase (IC₅₀ = 0.2 μM); blocks LPS-mediated expression of inflammatory mediators at 10-20 μM and blocks NF-κB signaling; has applications in rheumatoid arthritis.