Mazindol was developed as an appetite suppressant. It exists in a dynamic equilibrium between three isomers (the keto and the R and S–ol forms, respectively) with the R or S–ol being the only relevant forms at physiologic pH. Both S- and R-mazindol supposed to target human serotonin and dopamine transporters. R-mazindol is the biologically relevant enantiomer.

Reserpic acid, a derivative of the antihypertensive drug reserpine, can inhibit norepinephrine uptake although it is much less effective than reserpine itself. Recently was shown, that reserpic acid possessed a strong binding to the pancreatic lipase, a major target for controlling the obesity.

Reserpic acid, a derivative of the antihypertensive drug reserpine, can inhibit norepinephrine uptake although it is much less effective than reserpine itself. Recently was shown, that reserpic acid possessed a strong binding to the pancreatic lipase, a major target for controlling the obesity.

Lobelanidine is one of lobelia alkaloids that are the constituents of Lobelia inflata. Lobelia Chinensis Lour. (L. chinensis) is a plant of the Campanulaceae family that is commonly known as "xi-mi-cao", and "she-she-cao". It has been widely used as an antidote, diuretic, and hemostat in traditional Chinese medicine for decades. Lobelanidine is known for its emetic and anticancer activity.

Lobelanidine is one of lobelia alkaloids that are the constituents of Lobelia inflata. Lobelia Chinensis Lour. (L. chinensis) is a plant of the Campanulaceae family that is commonly known as "xi-mi-cao", and "she-she-cao". It has been widely used as an antidote, diuretic, and hemostat in traditional Chinese medicine for decades. Lobelanidine is known for its emetic and anticancer activity.

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.

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.

Pseudopelletierine is the main alkaloid derived from the root-bark of the pomegranate tree (Punica granatum). Pseudopelletierine is used as an enzyme substrate.

Pseudopelletierine is the main alkaloid derived from the root-bark of the pomegranate tree (Punica granatum). Pseudopelletierine is used as an enzyme substrate.