(-)-DDMS (S-Didesmethylsibutramine, (S)-DDMS) is one of sibutramine active metabolites. Sibutramine is widely used in the treatment of obesity. Sibutramine acts by inhibiting the reuptake of serotonin and noradrenaline in synapses, thereby enhancing both satiety and energy expenditure. In preclinical models (S)-Didesmethylsibutramine affected locomotor behavior and the Porsolt test but appeared to be completely inactive on food intake. (S)-enantiomers of didesmethylsibutramine may, to some extent, contribute to sibutramine’s side effect profile.

The components of several Petasites species have been investigated and shown to include petasin furanopetasin derivatives belonging to the eremophilane type of sesquiterpene, and bakkenolide derivatives. It has been reported that the petasin derivatives have spasmolytic properties and bakkenolide-A has cytotoxic activity. Natural is (+)-isopetasol. It was also isolated from the rhizomes of Ligularia fischeri grown in Henan province of China. Isopetasol derivatives with an unsaturated acid ester moiety will selectively inhibit RNA synthesis in the ascites tumor of mouse.

Byzantionoside B was isolated from the aerial parts of Stachys byzantina as the C-9 epimer of blumenol C glucoside. Byzantionoside B showed osteogenic activity by increasing alkaline phosphatase activity and calcium contents to regulate differentiation and mineralization in human osteoblast cells.

Norboletone (INN) (former proposed brand name Genabol), or norbolethone, is an anabolic steroid that was never marketed. It was first developed in 1966 by Wyeth Laboratories, and tested for use as an agent to encourage weight gain and for the treatment of short stature, but was never marketed commercially because of fears that it might be toxic. Norboletone is on the World Anti-Doping Agency's list of prohibited substances, and is therefore banned from use in most major sports.

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.

GRI977143, a prototypic nonlipid agonist specific to the lysophosphatidic acid-2 LPA(2) receptor subtype, displays antiapoptotic activity and activates the ERK1/2 prosurvival pathway.

Ascomycin 19-epimer is a stereoisomer of ascomycin (immunomycin). Ascomycin was isolated in the early sixties as a fermentation product of Streptomyces hygroscopicus var. ascomycetus and probed for its antifungal activity. Ascomycin derivatives represent a novel class of anti-inflammatory macrolactams currently under development for the treatment of skin diseases.

Immunomycin (Ascomycin, FR-900520, FK520) is a macrocyclic lactone produced by S. hygroscopicus. It is well known as an antifungal and antibiotic agent. Immunomycin is an analog of FK506 and also contains a 23-membered ring. Both FK506 and Immunomycin bind to FKBP12 at the same binding site for hindering calcineurin. Thus, Immunomycin possesses immunosuppressive activity similar to that of FK506. It appears that Immunomycin inhibits the production of Th1 (interferon- and IL-2) and Th2 (IL-4 and IL-10) cytokines. Additionally, Immunomycin preferentially inhibits the activation of mast cells, an important cellular component of the atopic response. Immunomycin produces a more selective immunomodulatory effect in that it inhibits the elicitation phase of allergic contact dermatitis but does not impair the primary immune response when administered systemically. Immunomycin is a member of the polyketide group of compounds. The polyketide synthase (PKS) enzyme is used to produce polyketides. The preparation of polyketide compounds has low product yield with traditional chemical methodology using wild-type cells. Reeves et al. provide a novel method of preparing a polyketide using a host cell with a recombinant DNA vector. The recombinant DNA vector contains nucleic acids that can encode the Immunomycin PKS enzyme. Immunomycin synthesized using this technology yields PKS at higher levels than that achieved by PKS in nature.

Alloyohimbine is an alkaloid, a stereoisomer of yohimbine extracted from Rauvolfia serpentina. Alloyohimbine is a selective antagonist of alpha2-adrenoreceptor.

ES936 is a potent mechanism-based inhibitor of NAD(P)H:quinone oxidoreductase 1 (NQO1), that exhibited potent growth inhibition effects against human pancreatic cancer cell lines. It was also shown, that drug can stimulate DNA synthesis in some cells through a mechanism involving p38 MAPK.