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…

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…

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.

A dipyridinyl compound that demonstrates high in vitro and ex vivo selectivity for COX-2 over COX-1.

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.

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

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

A constituent of the Chinese herb Artemisia identified as having anticoagulant, hypolipidemic, vasorelaxant, antioxidant, and anti-inflammatory actions in experimental models.

An acyclic nucleoside phosphonate that acts as a reverse transcriptase inhibitor; demonstrates antiviral activity against herpes viruses, hepatitis B virus, and HIV in animal and clinical models of infections.

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 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.

A selective, ATP-competitive inhibitor of CK2 with Ki values ranging from 0.5-1 µM.

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.

A high-affinity, lipophilic, non-selective ligand of the β-adrenergic receptors (Kis = 0.114 and 0.4 nM for β2- and β3-adrenoceptors, respectively); acts as a receptor antagonist (beta blocker) or inverse agonist for β1 and β2 receptors but functions as an agonist at the…

A nitrogen mustard alkylating agent used as a chemotherapeutic agent against advanced transitional cell carcinoma; serves as a prodrug that is metabolized to its active DNA alkylating form, isophosphoramide mustard.