JWH-073, a synthetic cannabinoid, is an analgesic chemical from the naphthoylindole family that acts as a neutral antagonist of CB1 cannabioid receptor and binder of CB2 cannabinoid receptor. JWH-073 is being used as a recreational drug in Spice products, and is a controlled substance in USA.

Nitracaine, a new psychoactive substance, a structural analog of the dopamine reuptake inhibitor, dimethocaine; intended for research applications. The physiological and toxicological properties of this compound are still not known.

Pteropodine is a heterohimbine-type oxindole alkaloid specifically isolated from ‘Cat’s claw’ (Uncaria tomentosa), a plant that has shown cytostatic, anti-inflammatory and antimutagenic properties and is used in traditional medicine to cure a number of diseases. Pteropodine positively modulate the function of rat muscarinic M1 and 5-HT2 receptors expressed in Xenopus oocyte but further studies are necessary to elucidate the exact mechanism by which Pteropodine positively modulates muscarinic M1 and 5-HT2 receptor functions. Pteropodine reduced the sister-chromatid exchanges and micronucleated polychromatic erythrocytes production by doxorubicin in mouse, showing a protective effect on the in vivo DNA damage. Pteropodine exhibited a significant pro-apoptotic effect on Medullary thyroid carcinoma cells. Moreover, anti-proliferative effect of pteropodine was demonstrated on the acute lymphoblastic leukaemia cells and ovarian carcinoma cells.

P-88-8991 (Hydroxy Iloperidone, 4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl] propoxy]- 3-methoxy-methylbenzenemethanol) is the major active metabolite of Iloperidone an atypical antipsychotic that used for the acute treatment of schizophrenia in adults. Metabolic reduction of Iloperidone carbonyl group leads to P-88-8991 in rats, dogs, and humans. The receptor affinity profile of P-88-8991 is comparable to that of iloperidone: this metabolite binds to the serotonin 5-HT2A receptors, adrenergic alpha1 and alpha2C receptors, and D2A receptors and with lower affinity to other monoamine (dopamine, serotonin, and histamine H1 ) receptors. The comparable receptor binding profile of P-88-8991 indicates that it is likely to contribute to the clinical profile of iloperidone. Preclinical experiments, such as the mouse apomorphine climbing test, the rat self-stimulation, and the pole climb avoidance task, indicate antipsychotic activity of P88-8991 and confirm that this metabolite crosses the blood–brain barrier

Cryptotanshinone is one of the major tanshinones isolated from the roots of the plant Salvia miltiorrhiza Bunge (Danshen). Danshen has been widely used in traditional Chinese medicine for treatment of a variety of diseases, including coronary artery disease, acute ischemic stroke, hyperlipidemia, chronic renal failure, chronic hepatitis, and Alzheimer's disease, showing no serious adverse effects. Recent studies have shown that cryptotanshinone not only possesses the potential for treatment and prevention of the above-mentioned diseases, but also is a potent anticancer agent. In vitro studies have demonstrated that cryptotanshinone inhibits cell proliferation in a variety of cancer cell lines, including rhabdomyosarcoma, melanoma, cervical, colon, breast and prostate cancer cells. It has been described that cryptotanshinone induced a G1/G0 cell cycle arrest in rhabdomyosarcoma (Rh30) and prostate cancer (DU145) cells by downregulating expression of cyclin D1 and phosphorylation of retinoblastoma protein (Rb), but induced a G2/ M cell cycle arrest in melanoma (B16) cells via upregulating expression of Cdc25c, cyclin A1 and cyclin B1. Cryptotanshinone inhibiting expression of Aurora A kinase led to significant suppression of prostate cancer cells in vitro and in mice. Cryptotanshinone also induces cell death in cancer cells.

Iridoid glycoside gardenoside is the main effective extraction of Gardenia jasminoides Ellis, which is an indigenous medicinal herb widely used for hepatoprotective, analgesic, and antipyretic drug. Gardenoside was shown to be effective toward HCl/ethanol induced gastric injury in mice and prevents cellular steatosis.

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.

MCN-5652W68 is pharmacologically inactive enantiomer of an selective serotonin reuptake MCN-5652. The enantiomers of McN-5652 differed in their ability to inhibit ex vivo binding of paroxetine in rat frontal cortex and hypothalamus, in vitro uptake of 5-HT in rat blood platelets, and 5-HT-induced contraction of rat vascular smooth muscle, with (+)-McN-5652-Z being most active. No difference was observed between the effects of (+)- and (-)-McN-5652-Z on 5-HT metabolism by rat brain monoamine oxidase. MCN-5652, as enantiomeric mixture, is currently being used for positron emission tomography studies.

SL651498 was identified as a drug development candidate from a research program designed to discover subtype-selective GABA(A) receptor agonists for the treatment of generalized anxiety disorder and muscle spasms. SL651498 displayed high affinity for GABA(A) receptors containing alpha(1) and alpha(2 subunits, and weaker affinity for alpha5-containing GABA(A) receptors, it behaved as a full agonist at recombinant t GABA(A) receptors containing alpha(2) and alpha(3) subunits, and as a partial agonist at recombinant GABA(A) receptors expressing alpha(1) and alpha(5) subunits. It was shown, that SL651498 represented a promising alternative to agents currently used for the treatment of anxiety disorders and muscle spasms without the major side effects seen with classical benzodiazepines).

AH-7921 (3,4-Dichloro-N-([1-(dimethylamino)cyclohexyl] methyl)benzamide) is an N-substituted cyclohexylmethylbenzamide classified as an opioid analgesic with high addictive liability. The compound acts as an agonist of μ-opioid receptors, although at high doses it can also stimulate κ-opioid receptors. In animal studies, AH-7921 produced typical morphine-like actions, i.e., antinociception, respiratory depression, sedation, miosis, inhibition of gut propulsion, and lowered body temperature, with a potency almost equipotent to that of morphine. There is limited information available on the routes of administration and the doses of AH-7921 used. The compound is taken orally, nasally, by smoking, and, less commonly, by intravenous injection. Minimal oral effective doses for complete pain suppression by AH 7921 are 1.25 and 13.8 mg/kg for canine and rhesus monkey, respectively.