The major estrogen secreted by the premenopausal ovary.

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…

A PPARα agonist and hypolipidemic drug used clinically to treat dyslipidemia and cardiovascular disease; exhibits EC50 values of 18 and 30 µM for mouse and human PPARα, respectively.

Diethylstilbestrol (DES) is a synthetic estrogen receptor agonist that was prescribed to pregnant women in the late 1930s. It was banned in 1971 because of possible links to increased risk of breast cancer in mothers along with congenital abnormalities and increased risk of cancer in offspring. DES…

Bezafibrate is a well established pan-PPAR activator. This fibrate drug has over 25 years of therapeutic use with a good safety profile. The fibrate class of drugs are generally known as PPARα agonists, but bezafibrate appears to activate PPAR.delta. and PPARγ as well. Bezafibrate…

A long-chain saturated fatty acid that does not affect plasma total cholesterol or LDL-cholesterol but may reduce HDL-cholesterol.

Saturated fatty acids are synthesized by both plants and animals from acetyl coenzyme A as a form of long-term energy storage. Palmitic acid is a common 16-carbon saturated fat that represents 10-20% of the normal human dietary fat intake, and approximately 25% of the total plasma fatty acids in…

A methyl ester prodrug form of the NOS inhibitor L-NNA; exhibits Ki values of 15 nM, 39 nM, and 4.4 µM for nNOS (bovine), eNOS (human), and iNOS (mouse), respectively.

An isoflavonoid phytoestrogenic compound found in soybeans, pea pods, clover, kudzu, and other legumes.

A major flavonolignan from the extracts of milk thistle seed, S. marianum; blocks the production of superoxide in PMA-activated rat Kupffer cells (EC50 = ~100 µM); inhibits the synthesis of LTB4 (IC50 = ~15 µM).

A progestin that is a racemic mixture of which levonorgestrel is the biologically active component.

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…

Palmitic acid ethyl ester is a neutral, lipid-soluble form of the free acid. It is one of the fatty acid ethyl esters that increase cytosolic Ca2+ concentration leading to pancreatic acinar cell injury due to excessive consumption of ethanol.

A non-selective NSAID exhibiting IC50 values of 0.5 and 2.33 µM for human recombinant COX-1 and COX-2, respectively.

A potent PR and GR antagonist with Ki value of approximately 1 nM.

(S)-Naproxen is a non-selective COX inhibitor. The IC₅₀ values for human recombinant COX-1 and -2 are 0.6-4.8 µM and 2.0-28.4 µM, respectively.

A flavonoid compound found in the bark and rinds of many plants and fruits.

A time-dependent, non-specific COX inhibitor with IC₅₀ values of 1.5 and 9.7 µM for human recombinant COX-1 and COX-2, respectively.

A synthetic glucocorticoid that binds the human glucocorticoid receptor with a higher affinity than a natural ligand, cortisol (Kd = 5 vs. 17 nM, respectively); has anti-inflammatory effects.

Chlorogenic acid is a phenolic natural product isolated from the leaves and fruits of dicotyledonous plants, including the coffee bean. Structurally, chlorogenic acid is the ester of caffeic acid with the 3-hydroxyl group of quinic acid. Chlorogenic acid is an important factor in plant metabolism.…

Estrone is one of the three naturally occurring estrogens, the others being estradiol and estriol. Estrone is synthesized from androstenedione by the aromatase enzyme system in the ovaries and placenta, and is also synthesized from estradiol by 17-hydroxy steroid dehydrogenase in the liver. Serum…

A synthetic intermediate or building block for drug discovery or pharmaceutical synthesis.

Hydroxymethyl uracil is a product of oxidative damage to DNA, predominantly by hydroxyl radical via the Fenton reaction.

An alkaloid natural product that reduces total cholesterol, LDL cholesterol, and triglycerides in humans and hamsters; enhances LDL-receptor protein and mRNA levels in hepatocytes.

A synthetic intermediate useful for pharmaceutical synthesis.

Nitroxyl (HNO) is the one electron reduced form of nitric oxide. Piloty’s acid is one of the best known and most widely used HNO donors. Under basic conditions Piloty’s acid decomposes to HNO and benzenesulfinate anion. The rate of HNO release at pH 7 is very slow (t½ = 5500…

A synthetic analog of 17β-estradiol

Traumatic acid is a product of the hydroperoxide lyase pathway in plants. It is a wound healing agent that stimulates cell division near a wound site to form a protective callus.

Nitrotyrosine is formed by peroxynitrite-mediated nitration of protein tyrosine residues. Its presence on proteins can be used as a marker for peroxynitrite formation in vivo. Both free and protein-bound nitrotyrosine are commonly found in mammalian tissues and are increased in pathological…

An estradiol analog that binds to ERα with IC50 values in the range of 22-28 nM

TMPD is an easily oxidizable compound that serves as a reducing co-substrate for heme peroxidases. TMPD undergoes one-electron oxidation by the heme peroxidase higher oxidation states (compounds I and II) producing a highly colored product that absorbs at 611 nm. Thus, the stoichiometry of…

An amide of docosenoic acid first identified in the CSF of sleep-deprived cats; causes reduced mobility and slightly lessened awareness in rats.