Unsolved:Actoprotector

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Short description: Type of compound

Actoprotectors or synthetic adaptogens are compounds that enhance bodily resilience to physical stress without increasing heat output.[1] Actoprotectors are distinct from other compounds that increase physical and psychological in their non-exhaustive action.[1] The term "actoprotector" is used to describe synthetic and isolated compounds possessing apoptogenic properties. By contrast, the term "adaptogen" is most often use to describe a natural herb as a whole, which can contain hundreds if not thousands of biologically active components.[2]

Distinction from psychostimulants

The term actoprotector was coined to distinguish between the pharmacologically distinct mechanism of action of psychostimulant drugs (especially phenethylamines) and actoprotectors. Drugs of both classes increase resiliency, but actoprotectors are presumed to do so via non-exhaustive action.

For example, at least part of the action of bromantane on improving physical resiliency is mediated by upregulation of tyrosine hydroxylase, thereby increasing dopaminergic signaling in the brain.[3] By contrast, the action of amphetamine (a phenethylamine psychostimulant) on improving physical resiliency is mostly mediated by induction of dopamine and norepinephrine release from the neuronal vesicles.[4]

Criteria

In a similar fashion to the term nootropic, the term actoprotector maintains various criteria.

  1. Have minimal [direct] pharmacological activity on biological receptors.[1]
  2. Facilitate rapid recovery (by reducing central nervous system fatigue).[1]
  3. Most effective in individuals with low to moderate baseline resilience to stress.[1]
  4. Involve a complexity of biochemical processes.[1]
  5. Decrease entropy of an organism (lowering oxygen consumption, body temperature, heart rate, etc).[1]
  6. Possess efficacy that is independent of extreme conditions.[1]
  7. Possess the ability to modify the pathology of pathogenic therapy agents (see memantine's use for influenza).[1]

Some compounds may possess actoprotector properties in some areas of their mechanism of action, while not being actoprotectors themselves. For example, the atypical stimulant modafinil appears to dampen amygdala activity independent of its dopaminergic effect,[5][6] resulting in a non-exhaustive increase in stress tolerance.[5]

Actoprotector structures.png

Chemical structure

Most actoprotectors fall into one of two groups depending on their chemical structure:[7]

- Benzimidazole derivatives such as Bemitil

- Adamantane derivatives such as Bromantane

List of actoprotectors

References

  1. 1.0 1.1 1.2 1.3 1.4 1.5 1.6 1.7 1.8 "The pharmacology of actoprotectors: practical application for improvement of mental and physical performance". Biomolecules & Therapeutics 20 (5): 446–456. September 2012. doi:10.4062/biomolther.2012.20.5.446. PMID 24009833. 
  2. "Refections Paper on the Adoptogenic Concept". European Medicines Agency. 8 May 2008. https://www.ema.europa.eu/en/documents/scientific-guideline/reflection-paper-adaptogenic-concept_en.pdf. 
  3. Morozov, I. S.; Ivanova, I. A.; Lukicheva, T. A. (2001-05-01). "Actoprotector and Adaptogen Properties of Adamantane Derivatives (A Review)" (in en). Pharmaceutical Chemistry Journal 35 (5): 235–238. doi:10.1023/A:1011905302667. ISSN 1573-9031. https://doi.org/10.1023/A:1011905302667. 
  4. Martin, Dustin; Le, Jacqueline K. (2022), "Amphetamine", StatPearls (Treasure Island (FL): StatPearls Publishing), PMID 32310563, http://www.ncbi.nlm.nih.gov/books/NBK556103/, retrieved 2022-08-18 
  5. 5.0 5.1 Rasetti, Roberta; Mattay, Venkata S; Stankevich, Beth; Skjei, Kelsey; Blasi, Giuseppe; Sambataro, Fabio; Arrillaga-Romany, Isabel C; Goldberg, Terry E et al. (September 2010). "Modulatory Effects of Modafinil on Neural Circuits Regulating Emotion and Cognition". Neuropsychopharmacology 35 (10): 2101–2109. doi:10.1038/npp.2010.83. ISSN 0893-133X. PMID 20555311. PMC 3013347. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3013347/. 
  6. van Vliet, Sanneke A. M.; Jongsma, Marjan J.; Vanwersch, Raymond A. P.; Olivier, Berend; Philippens, Ingrid H. C. H. M. (2006-05-01). "Behavioral effects of modafinil in marmoset monkeys" (in en). Psychopharmacology 185 (4): 433–440. doi:10.1007/s00213-006-0340-4. ISSN 1432-2072. https://doi.org/10.1007/s00213-006-0340-4. 
  7. Oliynyk, Sergiy; Oh, Sei-Kwan (2012-09-30). "The Pharmacology of Actoprotectors: Practical Application for Improvement of Mental and Physical Performance" (in en). Biomolecules and Therapeutics 20 (5): 446–456. doi:10.4062/biomolther.2012.20.5.446. ISSN 1976-9148. PMID 24009833. PMC 3762282. http://koreascience.or.kr/journal/view.jsp?kj=OOOMB4&py=2012&vnc=v20n5&sp=446.