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File:TAAR1 Dopamine.svg

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English: This is an illustration of a dopamine neuron with colocalized trace amine-associated receptor 1 (TAAR1) and the effects of a TAAR1 agonist (amphetamine or a trace amine like phenethylamine) on dopamine reuptake and effluxion. In technical terms, this is the pharmacodynamics of amphetamine and phenethylamine in this type of neuron.

This model was based upon information from the three following sources:

  1. Wimalasena K (July 2011). "Vesicular monoamine transporters: structure-function, pharmacology, and medicinal chemistry". Med Res Rev 31 (4): 483–519. doi:10.1002/med.20187. PMC 3019297. PMID 20135628
  2. Miller GM (January 2011). "The emerging role of trace amine-associated receptor 1 in the functional regulation of monoamine transporters and dopaminergic activity". J. Neurochem. 116 (2): 164–176. doi:10.1111/j.1471-4159.2010.07109.x. PMC 3005101. PMID 21073468.
  3. Eiden LE, Weihe E (January 2011). "VMAT2: a dynamic regulator of brain monoaminergic neuronal function interacting with drugs of abuse". Ann. N. Y. Acad. Sci. 1216: 86–98. doi:10.1111/j.1749-6632.2010.05906.x. PMID 21272013.

Supplemental citation with additional coverage of VMAT2 inhibition by phenethylamine:

  • Offermanns, Stefan; (eds.), Walter Rosenthal (2008). Encyclopedia of Molecular Pharmacology (2nd ed. ed.). Berlin: Springer. pp. 1219–1222. ISBN 3540389164.


In this diagram, amphetamine enters the presynaptic neuron across the neuronal membrane or through the dopamine transporter (DAT). Once inside, it binds to TAAR1 or enters synaptic vesicles through vesicular monoamine transporter 2 (VMAT2). When amphetamine or a trace amine binds to TAAR1, it reduces postsynaptic dopamine neuron firing rate (via mechanisms that are not shown) and triggers protein kinase A (PKA) and protein kinase C (PKC) signaling, resulting in DAT phosphorylation. Phosphorylated DAT then either operates in reverse or withdraws into the presynaptic neuron and ceases transport. When amphetamine or a trace amine enters the synaptic vesicles through VMAT2, dopamine is released into the cytosol (light tan area).
Date Original version:17 February 2014
Current version: 5 April 2017
Source Own work
Author Seppi333
Other versions PNG version: File:TAAR1 Amphetamine Dopamine.png
 
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Date/TimeThumbnailDimensionsUserComment
current23:25, 5 April 2017Thumbnail for version as of 23:25, 5 April 2017725 × 920 (202 KB)Seppi333 (talk | contribs)fixed text rendering issue from the last upload
23:18, 5 April 2017Thumbnail for version as of 23:18, 5 April 2017725 × 920 (202 KB)Seppi333 (talk | contribs)Fixed a minor error in a label
06:55, 29 January 2016Thumbnail for version as of 06:55, 29 January 2016725 × 920 (202 KB)Seppi333 (talk | contribs)tweak wording
08:26, 17 April 2015Thumbnail for version as of 08:26, 17 April 2015725 × 920 (203 KB)Seppi333 (talk | contribs)Changing the color of the cytosol for consistency with File:ΔFosB.svg; no other changes made.
04:38, 1 March 2014Thumbnail for version as of 04:38, 1 March 2014725 × 920 (203 KB)Seppi333 (talk | contribs)Fix text glitch
01:59, 1 March 2014Thumbnail for version as of 01:59, 1 March 2014725 × 920 (203 KB)Seppi333 (talk | contribs)Fix graphics glitch
01:57, 1 March 2014Thumbnail for version as of 01:57, 1 March 2014725 × 920 (195 KB)Seppi333 (talk | contribs)more tweaks
01:52, 1 March 2014Thumbnail for version as of 01:52, 1 March 2014725 × 920 (203 KB)Seppi333 (talk | contribs)FP feedback tweaks
21:22, 25 February 2014Thumbnail for version as of 21:22, 25 February 2014725 × 920 (191 KB)Seppi333 (talk | contribs)Cropping width...hoping for no more bugs
21:12, 25 February 2014Thumbnail for version as of 21:12, 25 February 2014740 × 915 (181 KB)Seppi333 (talk | contribs)+1 more to the massive column of files I've uploaded (attempt to fix edge clipping)
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