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ASR-2001

From Wikipedia, the free encyclopedia

Pharmaceutical compound
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-hallucinogenicserotonin5-HT2A receptor and5-HT1B receptoragonist
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
PubChemCID
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 as2CB-5PrO or as4-bromo-2-methoxy-5-propoxyphenethylamine, is a non-hallucinogenicserotonin receptor agonist of thephenethylamine,2C, andTWEETIO families which is under development for the treatment ofpsychiatric disorders.[2][3][4][5][6][7] It is the TWEETIOanalogue of2C-B in which the 5-methoxy group is replaced with a 5-propoxy group.[5][8] The drug is takenorally.[1]

Use and effects

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According to its developers, ASR-2001 has no overtpsychedelic effects, but instead produces a "focusing-type" "state of mental clarity" without the frankpsychostimulant effects of drugs likeamphetamine andmethylphenidate.[3][4][1][9] It is said to affectmood,concentration, andfocus, to not disturb but to potentially facilitate detailed work, and to capture the effects that are being sought withpsychedelic microdosing but with less risk.[9][1] As an example of its bettersafety profile, there is aceiling 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 thetoxic serotonin 5-HT2B receptor, in contrast to classical psychedelics likeLSD andpsilocybin.[9] ASR-2001 is said to have adose range of 10 to 40 mg, anonset of 1 to 1.5 hours, and aduration of 8 to 10 hours.[1] Itspsychoactive effects are described as "subtle".[1]

Interactions

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See also:Psychedelic drug § Interactions, andTrip killer § Serotonergic psychedelic antidotes

Pharmacology

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Pharmacodynamics

[edit]

ASR-2001 is a non-hallucinogenicserotonin5-HT2A receptoragonist and isorally active, highlypotent, and has highselectivity over the serotonin5-HT2B receptor (94-fold in terms ofactivational potency).[3][4][5][1][9][8] It is also a highly potent agonist of the serotonin5-HT1B receptor, whereas its activity at the serotoninserotonin5-HT1A receptor was very weak and its activity at the serotonin5-HT2C receptor was not described.[8] ASR-2001 showed no significant activity at a variety of other sites, including otherserotonin receptors and themonoamine transporters.[8] The drug is said to have lowefficacy in terms of serotonin 5-HT2A receptor activation, and this is said to be responsible for its lack of hallucinogenic effects.[9]

Development

[edit]

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

See also

[edit]

References

[edit]
  1. ^abcdefghijkGoldstein L (10 July 2023)."Pioneering Psychedelics Scientist Alexander "Sasha" Shulgin's Legacy Lives On Via New Compounds And Research".Benzinga. Retrieved19 April 2025.
  2. ^abc"Delving into the Latest Updates on ASR-2001 with Synapse".Synapse. 5 April 2025. Retrieved19 April 2025.
  3. ^abcdeBusby M (2 November 2023)."The Heirs to a Vault of Novel Psychedelics Take a Trip Into the Unknown".DoubleBlind Mag. Retrieved19 April 2025.
  4. ^abcdBusby M (30 March 2025)."What Happens When You Inherit 500 Psychedelic Compounds?".DoubleBlind Mag. Retrieved19 April 2025.
  5. ^abcdKargbo 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. Retrieved19 April 2025.
  7. ^abMichael Haichin (2024)."Psychedelics Drug Development Tracker".Psychedelic Alpha. Retrieved29 January 2025.
  8. ^abcdeWO patent 2024243599A1, Mark J. Martini; Nicholas V. Cozzi & Paul F. Daley et al., "Asymmetric phenylalkylamines", published 28 November 2024, assigned toAlexander Shulgin Research Institute 
  9. ^abcdefgJoe 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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