In June of 1993 Daniel Siebert discovered the strikingly powerful effects of salvinorin A, following the smoking of an extract which he had produced. Prior to producing the extract Siebert had been experimenting with ingestion of Salvia divinorum and smoking the dried leaves. Although these experiments allowed him to enter a psychedelic world, he felt that a much vaster dimension was waiting beyond the state produced by these methods of consumption. He began a series of experiments producing
concentrated extracts and trying various methods of administration, During his experiments, Siebert felt the plant's spirit was issuing a kind of intuitional guidance, encouraging him to continue with the extraction process and discover a means of achieving a full Salvia experience.

Pure salvinorin A is desirable because it permits one to experience intense psychedelic effects which are often elusive when using the whole plant material. In particular, when smoking dried Salvia divinorum leaf, many people fail to achieve more than a mild effect, although a few find this method quite satisfactory.

Upon his discovery of two terpenoid compounds, Valdes named them divinorin A and divinorin B. However, since Ortega had previously discovered and named the first of these compounds. the name salvinorin A is currently used for the plants primary terpenoid component. Salvinorin B, which represents about 4% of the plant's terpenoids, did not  turn out to be psychoactive in Valdes' animal studies, however, it has yet to be tested in humans. Valdes has also isolated other terpenoids from Salvia divinorum.
 

In his book, Pharmako/Poeia, Dale Pendell indicates that one may need to work with the plant for some time before feeling its effects.
 

"The Ally - She can be shy. Sometimes she has to get to know you for a while before she will come out and say hello. But once she appears, are there any who are more direct?"
 

Siebert found that leaves harvested during the warmer months of the year were at least twice as potent as those harvested during the winter. John Gruber of the Philadelphia College of Pharmacy and Science recently performed HPLC tests which yielded between 1.5 and 2.2 mg. salvinorin A per gram of dried Salvia divinorum leaf with lower amounts appearing in the stems and traces in the roots. Earlier experiments by Siebert have yielded up to 4.4 mg. salvinorin A per gram of dried leaf. The dried leaf equals approximately 13% of the fresh weight.

Siebert also discovered that when ingesting Salvia divinorum, its active components are absorbed primarily through contact with the oral mucosa. His  experiments  showed  that  significant  entheogenic experiences were produced by chewing 8 to 10 large fresh leaves (3 grams each, fresh weight) and holding them in the mouth for 10 minutes, while quickly swallowing the same amount of material produced no noticeable effects. In sessions where
Salvia divinorum was administered by Mazatecan shamans, most westerners who reported definite psychoactive effects were given 50 to 100 leaves. Reports on the plant's psychoactivity were inconsistent, and much of what was absorbed by those who felt its effects may have been through the oral mucosa during the process of chewing and consuming the leaves.

Shortly after discovering salvinorin A's effects, Siebert sent a sample to David Nichols who initiated a NovaScreen^TM receptor site screening. The screening results were in contrast to those of all previously tested psychedelics. Salvinorin A did not affect any of the receptor sites tested, which included all of the likely known receptor sites for other psychedelics.