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4-Bromomescaline

4-Bromomescaline, also known as 4-bromo-3,5-dimethoxyphenethylamine (4-Br-3,5-DMPEA), is a serotonin receptor modulator of the phenethylamine and scaline families related to the psychedelic drug mescaline. It is the analogue of mescaline in which the methoxy group at the 4 position has been replaced with a bromine atom. The drug is also the phenethylamine (α-desmethyl) analogue of 4-Br-3,5-DMA and a positional isomer of 2C-B (4-Br-2,5-DMPEA).

Use and effects

In his book PiHKAL (Phenethylamines I Have Known and Loved), Alexander Shulgin briefly mentions 4-bromomescaline and states that it has never been tested in humans. As such, its properties and effects in humans are unknown.

Pharmacology

Pharmacodynamics

4-Bromomescaline has been found to be a potent serotonin receptor agonist in the sheep umbilical artery ( = 185nM). It was 7.6-fold more potent than mescaline in this assay. In a subsequent study, the drug showed high affinity for the serotonin 5-HT<sub>2A</sub> receptor (K<sub>0.5</sub> = 45nM). Its affinity for this receptor was approximately 18-fold higher than that of mescaline.

Chemistry

Analogues

Analogues of 4-bromomescaline include mescaline, desoxy (4-desoxymescaline; 4-methylmescaline; 4-Me-3,5-DMPEA), 4-O-desmethylmescaline (desmethyl; 4-hydroxymescaline; 4-OH-3,5-DMPEA), 2C-B (4-Br-2,5-DMPEA), and 4-Br-3,5-DMA, among others. 4-Br-3,5-DMA has been found to be a potent psychoactive drug in humans, though it did not produce clear hallucinogenic effects at tested doses of 3 to 10mg orally and instead produced pronounced analgesic and tactile anesthetic effects among others. On the other hand, desoxy (4-methylmescaline), a positional isomer of 2C-D, is a psychedelic drug similarly to mescaline at doses of 40 to 120mg orally, albeit with distinct effects.

Daniel Trachsel has expressed great interest in scaline-related compounds of the formula 4-X-3,5-DMPEA without an oxygen atom at the 4 position like desoxy (4-methylmescaline; 4-Me-3,5-DMPEA) and 4-bromomescaline (4-Br-3,5-DMPEA). He has described a variety of theoretical compounds of this class that could be explored, such as desoxyescaline (DE; 4-ethylmescaline; 4-Et-3,5-DMPEA), desoxytrifluoromescaline (DTFM; 4-trifluoromethylmescaline; 4-TFM-3,5-DMPEA), desoxytrifluoroescaline (DTFE; 4-trifluoroethylmescaline; 4-TFE-3,5-TMPEA), desoxyproscaline (DPR; 4-propylmescaline; 4-Pr-3,5-TMPEA), desoxyallylescaline (DAL; 4-allylmescaline; 4-AL-3,5-TMPEA), and desoxymethallylescaline (DMAL; 4-methallylmescaline; 4-MeAL-3,5-TMPEA), among others.

History

4-Bromomescaline was first described in the scientific literature by David E. Nichols and Shulgin and colleagues in 1977. Subsequently, it was described by Shulgin in PiHKAL in 1991.

See also

References

External links