alpha-yohmbine (aka rauwloscine) is a diastereomer of yohimbine and shares many of the same properties. Rauwolscine acts as an alpha-2-adrenergic antagonist and is therefore used as an unregulated nutritional supplement for fat-burning and CNS stimulation. Rauwolscine is also an antagonist of the HT2B receptor and has been investigated for the potential to mitigate blood vessel spasms.

1-(2-methoxyphenyl)piperazine is an effective blocker of striatal dopaminergic receptors in rat brain and is apparently the simplest chemical structure known to exert dopaminergic blocking activity. It is exhibited pronounced antihypertensive and weak sympatholytic activities in experimental animals. Blood pressure was also lowered in hypertensive patients and this effect was sometimes accompanied by a strong sedation, and after large repeated doses, by disorientation and stupor. In a filter paper bioassay 1-(2-methoxyphenyl)piperazine demonstrated acaricidal activity. 1-(2-methoxyphenyl)piperazine is a building block of many serotonergic and dopaminergic agents. Some of them have antidepressant activity.

J 113863 is a potent and high selective CKR-1 (CCR1) and CKR-3 (CCR3) chemokine receptor antagonist, which is also behaved as a full agonist of CCR2 and as a very partial agonist of CCR5. This compound was investigated for the treatment of multiple sclerosis and rheumatoid arthritis, but the status of these studies are not known.

Diethylammonium p-aminobenzoate is a powerful heart stimulant, with considerable effect on the uterus. Diethylammonium p-aminobenzoate protected the heart from the poisoning caused by procaine, maxicaine or xylocaine, and also against high doses of procaine amide. The substance passes the blood-spinal fluid barrier but high doses are necessary to find it in the spinal fluid, where it appears later than in the other body fluids. Diethylammonium p-aminobenzoate reduces the spontaneous activity of mice.

(S)-Etifoxine is a first in class pain-relieving drug candidate, with the power of morphine and oxycodone, but without the addictive, sedative and GI side effects. (S)-etifoxine is an isomer, chemically isolated from Etifoxine (Stresam), an approved racemic drug (off patent) prescribed in Europe. Preclinical studies determined that the (S)-isomer of Stresam® ((S)-etifoxine) is a non-sedating anxiolytic. It was also discovered that (S)-etifoxine possesses highly potent analgesic activity comparable to morphine (the gold standard) which is consistent with Stresam®’s TSPO-mediated effects on chemotherapy-induced neuropathy and peripheral nerve injury. However, (S)-etifoxine does not display any of the negative side-effects associated with morphine. Even more notably, Stresam® has demonstrated peripheral nerve regeneration and functional recovery. It is believed that (S)-etifoxine will retain these same properties.

Rosavin is a glycoside found in the plant Rhodiola rosea. It is a component of rosavin capsules from Ameriden which are marketd to reduce stress and anxiety.

Dihydroisocodeine is an opioid derivative. Dihydroisocodeine is much less toxic for rabbits than codeine, and in these and other animals its convulsant action is less marked. The minimum analgesic dose for cats is considerably less than for codeine. In the 1930s it was clinically investigated for cough relief, where it has no demonstrable clinical superiority over standard codeine in the usual therapeutic dosage.

(R)-Aminoglutethimide is R-isomer of racemate anti-steroid drug Aminoglutethimide, marketed by Novartis for the treatment of Cushing syndrome and other conditions. (R)-Aminoglutethimide was shown to more active than (S)-isomer in inhibiting corticosteroid release in rats, more potent in inhibiting aromatization of testosterone by human placental microsomes. (R)-Aminoglutethimide was investigated in a clinical trial against breast cancer, where it was found to enhance the clearance rate of plasma estrone sulfate.

Caprospinol, also known as SP-233, a spirostenol derivative, protects neuronal cells against β-Amyloid (Abeta(1-42)) protein toxicity by binding to and inactivating this peptide. It was shown, that caprospinol crossed the blood-brain barrier, accumulated in the brain, and restored cognitive impairment in a pharmacological rat model of Alzheimer's disease. It was suggested, that the drug could be considered as a promising drug for Alzheimer's disease treatment.

α-peltatin is a lignan, which was isolated from different species of Linum and has been studied in patients with advanced neoplasms.