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 dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity; selectively inhibits adenosine A3 receptors (Ki = 3.25 µM) and CYP3A4 catalytic activity (IC₅₀ = 0.148 µM); activates TRPA1 channels, producing an increase in Ca2+…

A pyrimadine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis; widely used to treat many gastrointestinal tract adenocarcinomas.

An agonist of α2 adrenergic receptors (Ki = 194 nM); used for sedation, anesthesia, and analgesia in non-human mammals.

A classical inhibitor of complex I of the mitochondrial electron transport chain, inhibiting NADH/DB oxidoreductase and NADH oxidase with IC₅₀ values of 28.8 and 5.1 nM, respectively; used in animal models of Parkinson’s disease.

An isomer of hypoxanthine that inhibits xanthine oxidoreductase (IC50 values between 0.2 and 50 μM); lowers serum and urinary uric acid levels in vivo and is used to treat gout and hyperuricemia.

An NSAID that acts as a COX-2 inhibitor (IC₅₀s = 20 and 322 nM for COX-1 and COX-2, respectively).

An antimalarial drug used in the treatment of persistent liver forms of P. vivax or P. ovale infection for its ability to kill late-stage gametocytes and hypnozoites.

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 alkyl sulfonate that acts as an alkylating antineoplastic agent; forms both intra- and interstrand crosslinks on DNA, in addition to monoalkylation, primarily at guanine-N7, of DNA.

A selective agonist of GABAB (IC₅₀ = 200 nM); causes skeletal muscle relaxation and blocks spasticity.

A centrally acting M1 muscarinic acetylcholine receptor antagonist (Ki = 0.59 nM in rat) that also inhibits dopamine uptake through the dopamine transporter (Ki = 160 nM); used in the management of Parkinson’s disease symptoms to address involuntary tremor and dystonia.

A natural neurotransmitter that is activates adrenoceptors (Kis = 15, 735, and 3,970 nM for α1A-, β2-, and β1-adrenergic receptors, respectively); may induce either contraction or relaxation of vascular smooth muscle, depending on adrenoceptor subtype expression.

5-Chloroesorcinol dimethyl ether is a synthetic intermediate useful for pharmaceutical synthesis.

Niflumic acid is a selective inhibitor of COX-2. The IC₅₀ values are 16 and 0.1 µM for human recombinant COX-1 and -2, respectively. The Ki values are 2 and 0.02 µM for ovine COX-1 and -2, respectively.

A polypeptide antibiotic effective against Gram-negative bacteria, including P. aeruginosa, A. baumannii, and K. pneumoniae.