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ASR-2001
Clinical data
Other namesASR2001; 2CB-5PrO; 5-PrO-2C-B; 4-Bromo-2-methoxy-5-propoxyphenethylamine
Routes of
administration		Oral[1]
Drug classNon-hallucinogenic serotonin 5-HT2A receptor and 5-HT1B receptor agonist
ATC code
  • None
Pharmacokinetic data
Onset of action1–1.5 hours[1]
Duration of action8–10 hours[1]
Identifiers
  • 2-(4-bromo-2-methoxy-5-propoxyphenyl)ethanamine
PubChem CID
Chemical and physical data
FormulaC12H18BrNO2
Molar mass288.185 g·mol−1
3D model (JSmol)
  • CCCOC1=C(C=C(C(=C1)CCN)OC)Br
  • InChI=1S/C12H18BrNO2/c1-3-6-16-12-7-9(4-5-14)11(15-2)8-10(12)13/h7-8H,3-6,14H2,1-2H3
  • Key:SMMQLGYZANIEMB-UHFFFAOYSA-N

ASR-2001, also known as 2CB-5PrO or as 4-bromo-2-methoxy-5-propoxyphenethylamine, is a non-hallucinogenic serotonin receptor agonist of the phenethylamine, 2C, and TWEETIO families which is under development for the treatment of psychiatric disorders.[2][3][4][5][6][7] It is the TWEETIO analogue of 2C-B in which the 5-methoxy group is replaced with a 5-propoxy group.[5][8]

The drug is a non-hallucinogenic serotonin 5-HT2A receptor agonist and is orally active, highly potent, and has high selectivity over the serotonin 5-HT2B receptor (94-fold in terms of activational potency).[3][4][5][1][9][8] It is also a highly potent agonist of the serotonin 5-HT1B receptor, whereas its activity at the serotonin serotonin 5-HT1A receptor was very weak and its activity at the serotonin 5-HT2C receptor was not described.[8] ASR-2001 showed no significant activity at a variety of other sites, including other serotonin receptors and the monoamine transporters.[8] The drug is said to have low efficacy in terms of serotonin 5-HT2A receptor activation, and this is said to be responsible for its lack of hallucinogenic effects.[9]

According to its developers, ASR-2001 has no overt psychedelic effects, but instead produces a "focusing-type" "state of mental clarity" without the frank psychostimulant effects of drugs like amphetamine and methylphenidate.[3][4][1][9] It is said to affect mood, concentration, and focus, to not disturb but to potentially facilitate detailed work, and to capture the effects that are being sought with psychedelic microdosing but with less risk.[9][1] As an example of its better safety profile, there is a ceiling effect with ASR-2001 such that pushing the dose will not result in an accidental psychedelic experience.[9] In addition, the drug has strong selectivity over the toxic serotonin 5-HT2B receptor, in contrast to classical psychedelics like LSD and psilocybin.[9] ASR-2001 is said to have a dose range of 10 to 40 mg, an onset of 1 to 1.5 hours, and a duration of 8 to 10 hours.[1] Its psychoactive effects are described as "subtle".[1]

ASR-2001 is under development by Nicholas V. Cozzi and Paul F. Daley and colleagues at the Alexander Shulgin Research Institute (ASRI).[3][4][1][2] It was first described in 2023[1][3] and was patented in 2024.[5][8] As of early 2025, ASR-2001 is in the preclinical research stage of development.[7][2] Potential applications of ASR-2001 are said to include treatment of attention-deficit hyperactivity disorder (ADHD) and self-betterment in healthy individuals, depending on what regulatory agencies may allow.[9]

See also

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References

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  1. ^ a b c d e f g h i j Goldstein L (10 July 2023). "Pioneering Psychedelics Scientist Alexander "Sasha" Shulgin's Legacy Lives On Via New Compounds And Research". Benzinga. Retrieved 19 April 2025.
  2. ^ a b c "Delving into the Latest Updates on ASR-2001 with Synapse". Synapse. 5 April 2025. Retrieved 19 April 2025.
  3. ^ a b c d e Busby M (2 November 2023). "The Heirs to a Vault of Novel Psychedelics Take a Trip Into the Unknown". DoubleBlind Mag. Retrieved 19 April 2025.
  4. ^ a b c d Busby M (30 March 2025). "What Happens When You Inherit 500 Psychedelic Compounds?". DoubleBlind Mag. Retrieved 19 April 2025.
  5. ^ a b c d Kargbo RB (April 2025). "Innovative Approaches in Psychedelics, AI, and Communication: A Multi-Domain Perspective". ACS Med Chem Lett. 16 (4): 514–516. doi:10.1021/acsmedchemlett.5c00114. PMID 40236531.
  6. ^ "Alexander Shulgin Research Institute discovers new phenylalkylamine compounds". BioWorld. 19 December 2024. Retrieved 19 April 2025.
  7. ^ a b Michael Haichin (2024). "Psychedelics Drug Development Tracker". Psychedelic Alpha. Retrieved 29 January 2025.
  8. ^ a b c d e WO patent 2024243599A1, Mark J. Martini; Nicholas V. Cozzi & Paul F. Daley et al., "Asymmetric phenylalkylamines", published 28 November 2024, assigned to Alexander Shulgin Research Institute 
  9. ^ a b c d e f g Joe Moore (2 April 2024). "Shulgin Farm and the Future of Psychedelic Drug Development (Featuring: Paul F. Daley, Ph.D.)" (Podcast). Psychedelics Today. Event occurs at 16:12–20:45. We have a second lead compound that's a phenethylamine that is actually not psychedelic but it does have effects on mood, concentration, focus, and I've been saying that I think it sort of captures the effect that people are trying to achieve with microdosing, but on two accounts it has much better safety profile. If you push dose, since it has limited efficacy, that's how fully can the receptor systems that it touches be turned on, its efficacy appears to be low, so even if you push dose, there's sort of a ceiling of effect, and it never becomes really psychedelic. So that's a safety factor, you can't overdo it and be all of a sudden tripping at your desk, which is not necessarily a great outcome. [...] So this second compound that we call ASR-2001 is about 100-fold less effective at 2B than at 2A. [...]
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