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APA-01
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| Other names | APA01; APA-001; APA001; PharmAla-1; P-1; (R)-2-[(2H-1,3-benzodioxol-5-yl)methyl]pyrrolidine |
| Drug class | Entactogen |
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| Formula | C12H15NO2 |
| Molar mass | 205.257 g·mol−1 |
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APA-01, also known as PharmAla-1, is an entactogen of the phenethylamine, amphetamine, and MDxx families related to MDMA which is under development for potential medical use.[1][2][3][4] It is a cyclized phenethylamine and is a derivative of MDMA in which the α position has been cyclized with the amine via a propyl group to form a pyrrolidine ring.[2][3][4]
The drug is predicted to interact with the monoamine transporters and with the serotonin 5-HT2 receptors.[4] In contrast to MDMA, it does not produce hyperthermia in rodents, instead producing dose-dependent hypothermia.[4] In addition, unlike MDMA, neither APA-01 nor the corresponding (S)- enantiomer showed hyperlocomotion in rodents.[4] Both APA-01 and the (S)- enantiomer produced sympathomimetic cardiovascular effects in rodents, but APA-01 had reduced impact compared to the (S)- enantiomer and relative to MDMA and dextromethamphetamine.[4] APA-01 showed prosocial effects in rodents similarly to MDMA, but with greater potency.[4] The drug is said to have improved safety compared to MDMA.[2]
The chemical synthesis of APA-01 has been described.[4]
APA-01 is under development by PharmAla Biotech.[1][2][3][4] As of April 2026, it is in the preclinical research stage of development.[1] Possible medical applications of APA-01 include treatment of post-traumatic stress disorder (PTSD) and neurological conditions like traumatic brain injury (TBI) and stroke.[3] The drug was first described in the scientific literature, in a conference presentation, by 2024.[2]
See also
[edit]- Substituted methylenedioxyphenethylamine
- Cyclized phenethylamine
- List of investigational hallucinogens and entactogens
- 2-Benzylpiperidine
- MDPPP
- Non-racemic MDMA (ALA-002)
References
[edit]- ^ a b c "Delving into the Latest Updates on APA-01 with Synapse". Synapse. 8 May 2025. Retrieved 28 April 2026.
- ^ a b c d e Kaur H (26 September 2026). APA-01: Development of a Potent Entactogen with Improved Safety Pharmacology Compared to MDMA. European Behavioural Pharmacology Society (EBPS) Biennial Workshop, Banff, Alberta, Canada • 25-27 September 2024 [Novel Pharmacotherapies for Substance Use and Related Mental Health Disorders]. European Behavioural Pharmacology Society (EBPS).
- ^ a b c d PharmAla Biotech (27 April 2026). "PharmAla Executes Binding Letter of Intent for Formation of Special Purpose Vehicle to Develop Patented Novel MDXX Molecule APA-01". GlobeNewswire News Room (Press release). Retrieved 28 April 2026.
[...] APA-01 (also known as PharmAla-1 or "P-1"), the Company's patented novel MDXX molecule. [...] APA-01 is (R)-2-[(2H-1,3-benzodioxol-5-yl)methyl]pyrrolidine, a novel molecule protected by United States Patent No. 12,042,478, with potential therapeutic applications in the treatment of psychological trauma and neurological conditions, including Traumatic Brain Injury and Stroke. APA-01 is part of PharmAla's broader portfolio of novel MDXX class molecules being developed alongside its lead drug candidate, ALA-002, via its Phenesafe.AI drug discovery platform.
- ^ a b c d e f g h i US 12042478, Kaur H, Xin T, "(R)-2-[(2H-1,3-benzodioxol-5-yl)methyl]pyrrolidine and processes for preparation, compositions and uses thereof", published 15 February 2024, issued 23 July 2024, assigned to Pharmala Biotech Pharmala Biotech Inc.