2-Bromo-LSD, also known as BOL-148, is a derivative of
lysergic acid invented by
Albert Hofmann, as part of the original research from which the closely related compound
LSD was also derived.[3]
2-Bromo-LSD was found to be inactive as a
psychedelic and so was comparatively little researched for many years, although its similar behavior in the body made it useful for
radiolabelling studies. It was found to bind to many of the same
receptors as LSD, but acting as a
neutral antagonist rather than an agonist.[4][5] 2-Bromo-LSD reportedly attenuates the effects of LSD in humans.[6][7]
However its generally similar behavior to LSD in some respects has shown to be very useful in one specific area, the treatment of
cluster headaches.[8] These debilitating attacks have been known for some time to be amenable to treatment with certain hallucinogenic drugs such as LSD and
psilocybin, but because of the illegal status of these drugs and the kind of mental changes they induce, research into their medical use has been slow and therapeutic application limited to very specific circumstances under strict supervision. It had been thought that this specific therapeutic action against cluster headaches was limited to hallucinogenic drugs of this type, and would always present a major barrier to their clinical use. However, a serendipitous discovery found that 2-bromo-LSD can also produce this therapeutic effect, despite lacking the other effects of LSD. This has led to a resurgence of interest and research into 2-bromo-LSD and its possible medical uses. Some isolated incidents of hallucinogenic responses have been reported, but as with other non-hallucinogenic LSD analogs such as
lisuride, this appears to be a rare side effect occurring only in individuals with an as yet unexplained susceptibility to this reaction.
^Troxler F, Hofmann A (1957). "Substitutionen am Ringsystem der Lysergsäure. III. Halogenierung. 45. Mitteilung über Mutterkornalkaloide". Helvetica Chimica Acta. 40 (7): 2160–2170.
doi:
10.1002/hlca.19570400716.
^Karst M, Halpern JH, Bernateck M, Passie T (September 2010). "The non-hallucinogen 2-bromo-lysergic acid diethylamide as preventative treatment for cluster headache: an open, non-randomized case series". Cephalalgia. 30 (9): 1140–1144.
doi:
10.1177/0333102410363490.
PMID20713566.
S2CID33199115.
Dave KD, Harvey JA, Aloyo VJ (October 2007). "The time-course for up- and down-regulation of the cortical 5-hydroxytryptamine (5-HT)2A receptor density predicts 5-HT2A receptor-mediated behavior in the rabbit". The Journal of Pharmacology and Experimental Therapeutics. 323 (1): 327–335.
doi:
10.1124/jpet.107.121707.
PMID17640952.
S2CID13870625.
2-Bromo-LSD, also known as BOL-148, is a derivative of
lysergic acid invented by
Albert Hofmann, as part of the original research from which the closely related compound
LSD was also derived.[3]
2-Bromo-LSD was found to be inactive as a
psychedelic and so was comparatively little researched for many years, although its similar behavior in the body made it useful for
radiolabelling studies. It was found to bind to many of the same
receptors as LSD, but acting as a
neutral antagonist rather than an agonist.[4][5] 2-Bromo-LSD reportedly attenuates the effects of LSD in humans.[6][7]
However its generally similar behavior to LSD in some respects has shown to be very useful in one specific area, the treatment of
cluster headaches.[8] These debilitating attacks have been known for some time to be amenable to treatment with certain hallucinogenic drugs such as LSD and
psilocybin, but because of the illegal status of these drugs and the kind of mental changes they induce, research into their medical use has been slow and therapeutic application limited to very specific circumstances under strict supervision. It had been thought that this specific therapeutic action against cluster headaches was limited to hallucinogenic drugs of this type, and would always present a major barrier to their clinical use. However, a serendipitous discovery found that 2-bromo-LSD can also produce this therapeutic effect, despite lacking the other effects of LSD. This has led to a resurgence of interest and research into 2-bromo-LSD and its possible medical uses. Some isolated incidents of hallucinogenic responses have been reported, but as with other non-hallucinogenic LSD analogs such as
lisuride, this appears to be a rare side effect occurring only in individuals with an as yet unexplained susceptibility to this reaction.
^Troxler F, Hofmann A (1957). "Substitutionen am Ringsystem der Lysergsäure. III. Halogenierung. 45. Mitteilung über Mutterkornalkaloide". Helvetica Chimica Acta. 40 (7): 2160–2170.
doi:
10.1002/hlca.19570400716.
^Karst M, Halpern JH, Bernateck M, Passie T (September 2010). "The non-hallucinogen 2-bromo-lysergic acid diethylamide as preventative treatment for cluster headache: an open, non-randomized case series". Cephalalgia. 30 (9): 1140–1144.
doi:
10.1177/0333102410363490.
PMID20713566.
S2CID33199115.
Dave KD, Harvey JA, Aloyo VJ (October 2007). "The time-course for up- and down-regulation of the cortical 5-hydroxytryptamine (5-HT)2A receptor density predicts 5-HT2A receptor-mediated behavior in the rabbit". The Journal of Pharmacology and Experimental Therapeutics. 323 (1): 327–335.
doi:
10.1124/jpet.107.121707.
PMID17640952.
S2CID13870625.