Allyl- and Propargylamine Phenethylamines and Tryptamines for Tolerability
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Solution Overview
Problem
Current psychedelics and entactogens like LSD, psilocybin, and MDMA have limitations in therapeutic applications due to adverse reactions, varying tolerability profiles, and unsuitable pharmacological properties for some patients, necessitating the development of novel compounds with improved efficacy and reduced side effects for substance-assisted psychotherapy.
Innovation Solution
Development of phenethylamines and tryptamines with allyl- and/or propargylamine moieties that interact with serotonin 5-HT2A receptors and monoamine transporters, offering alternative therapeutic benefits with reduced adverse effects and tailored pharmacological profiles.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional psychedelics (LSD, psilocybin) and entactogens (MDMA) are used for substance-assisted psychotherapy, then therapeutic effects are achieved, but adverse reactions and varying tolerability profiles limit their applicability to some patients
Solution Approach 1:
The patent modifies the chemical structure of phenethylamines and tryptamines by changing parameters such as introducing allyl- and/or propargylamine moieties, substituting aromatic rings with heteroaromatic rings, and adding functional groups. These structural parameter changes result in novel compounds with improved pharmacological profiles, reduced adverse reactions, and enhanced tolerability while maintaining therapeutic efficacy for conditions like depression, anxiety, PTSD, and substance use disorders
2Adaptability or versatility
If existing psychedelics and entactogens are used, then psychoactive effects are produced, but unsuitable pharmacological properties for some patients necessitate development of novel compounds
Solution Approach 1:
The patent applies local quality by introducing specific functional groups and moieties (allyl- and propargylamine) at particular positions in the molecular structure. This localized modification allows tuning of specific pharmacological properties to match different therapeutic needs and patient requirements, enabling customized pharmacological profiles for various indications including depression, anxiety, PTSD, and substance use disorders
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
These compounds provide enhanced therapeutic effects with fewer side effects, improved tolerability, and tailored duration of action, addressing the limitations of existing psychedelics and entactogens in treating medical disorders.
Implementation Method 1
interacting with serotonin 5-HT2A receptors and/or with monoamine transporters in the mammal, and inducing psychoactive effects
Implementation Method 2
interacting with serotonin 5-HT2A receivers and/or with monoamine transporters in the mammal, and inducing psychoactive effects
Data Source
AI summary
A composition of a compound represented by FIGS. 1A-1E for use in treating a medical disorder. A method of changing neurotransmission, by administering a pharmaceutically effective amount of composition to a mammal of a compound represented by FIGS. 1A-1E and inducing psychoactive effects in the mammal. A method of treating a patient having adverse reactions to psychedelics or entactogens, by administering a pharmaceutically effective amount of composition to the patient of a compound represented by FIGS. 1A-1E and avoiding adverse effects present with psychedelics or entactogens.