Racemic phenibut (beta-phenyl-gamma-aminobutyric acid or 4-amino-3-phenylbutyric acid) is a neuropsychotropic drug that was discovered and introduced into clinical practice in Russia in the 1960s. In pharmacological tests of locomotor activity, antidepressant and pain effects, S-phenibut was inactive. In contrast, R-phenibut turned out to be two times more potent than racemic phenibut in most of the tests. Racemic phenibut and R-phenibut demonstrated an affinity for GABAB receptors, in contrast, S-phenibut was not able to bind receptors. Pharmacological activity of racemic phenibut relies on R-phenibut and this correlates to the binding affinity of enantiomers of phenibut to the GABAB receptor. Both S- and R-phenibut bind to the α2-δ subunit of voltage-dependent calcium channels and exert gabapentin-like anti-nociceptive effects. In addition S-isomer was found to be a substrate of gamma-aminobutyric acid aminotransferase, however, the R-isomer is a competitive inhibitor.

Napelline is a diterpenoid alkaloid, from plants of the Aconitum genus, Ranunculaceae. It is a potent antiarrhythmic of class I with weak hypotensive and N-cholinoblocking effects. Napelline has analgesic and anti-inflammatory activity. Napelline has a stronger antiarrhythmic activity than Quinidine or Procaïnamide. 10(-4) - 10(-5) M block inward Na+ currents

Epiestradiol is an estradiol isomer with weak estrogenic activity.

Meliltoside is a 2-glucosyloxycinnamic acid found in Dendrobium medicinal plants, Ajuga laxmannii, Ajuga chamaecistus ssp. tomentella, and Teloxys graveolens. It demonstrated moderate antiprotozoal and anti-cancer activity in vitro.