Serotonin–norepinephrine–dopamine reuptake inhibitor: Difference between revisions

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SNDRI compounds elevate extracellular concentrations of serotonin, norepinephrine and dopamine in the CNS.
These antidepressant compounds have Pharmacokinetics and Pharmacodynamics completely distinguishable from cocaine/amphetamine etc. Mostly, they dont function as psychostimulants. This is in strong agreement with some of the claims in the [[phenyltropane]] (RTI-112 etc).<br />
Technically speaking, [[Indatraline]] is a SNDRI, although it is not being actively persued in the context of a clinically useful antidepressant.<br />
psy·cho·stim·u·lant (sk-stmy-lnt)
n. A drug having antidepressant or mood-elevating properties. Well obviously I mean, er, LMA stimulant.
==Background==
==Background==
[http://www.ingentaconnect.com/content/ben/cnsnddt/2007/00000006/00000002 Depression (Part 1) Guest Editors: John H. Kehne and Ronald S. Duman (April 07)]
[http://www.ingentaconnect.com/content/ben/cnsnddt/2007/00000006/00000002 Depression (Part 1) Guest Editors: John H. Kehne and Ronald S. Duman (April 07)]

Revision as of 12:16, 10 April 2007

SNDRI compounds elevate extracellular concentrations of serotonin, norepinephrine and dopamine in the CNS.

Background

Depression (Part 1) Guest Editors: John H. Kehne and Ronald S. Duman (April 07)

The Genetics of Depression: A Review (Jul '06)

The Mesolimbic Dopamine Reward Circuit in Depression (Jun 06)

Serotonin Receptors as Targets in Drug Discovery and Medicinal Chemistry (Sep '06)

Serotonin-Dopamine Interaction as a Focus of Novel Antidepressant Drugs (feb 06)

Serotonin Reuptake Inhibitors: The Corner Stone in Treatment of Depression for Half a Century - A Medicinal Chemistry Survey.

Serotonin (5HT), Fluoxetine, Imipramine and Dopamine Target Distinct 5HT Receptor Signaling to Modulate Caenorhabditis elegans Egg-Laying Behavior Ji Ying Sze1 2005

DOV Compounds

(“Broad Spectrum” Antidepressants) Skolnick, Phil (April 2007)

Preclinical and clinical pharmacology of DOV 216,303, a "triple" reuptake inhibitor. Skolnick (2006)

DOV 216,303, a "Triple" Reuptake Inhibitor: Safety, Tolerability, and Pharmacokinetic Profile 04

Antidepressant-like actions of DOV 21,947: a “triple” reuptake inhibitor Phil Skolnick (2003)

“Broad spectrum” antidepressants: Is more better for the treatment of depression? Phil Skolnick (2003)

PRC Compounds

  • Notice the presence of a γ-amino-alcohol. Although, not immediately obvious to the novice, these are actually PEA derivatives.
  • Conditions required for PhCHO → Cyclohexanal: Hydrogen bomb.
File:Carlier.GIF

Antidepressant-like effects of novel triple reuptake inhibitors, PRC025 and PRC050 Paul R. Carlier and Elliott Richelson; Yiqun Zhang (2007)

Interactions of antidepressants with neurotransmitter transporters and receptors and their clinical relevance. Elliott Richelson (2003)

The clinical relevance of antidepressant interaction with neurotransmitter transporters and receptors. Richelson E. (2002)

  • PRC50 is species selective, it behaves differently in rats to humans, wrt DAT.
Eur.J.Pharmacology 555 (007) 30-36.
Compound hNAT Kd (nM) hNAT Ki (nM) hSERT Kd (nM) hSERT Ki (nM) hDAT Kd (nM) hDAT Ki (nM)
PRC0500.401.26.01212043
PRC02519106.06.010053
Venlafaxine10602109.03993005300
Paroxetine40330.130.734901700
Imipramine37141.441 850011000
Nomifensine16.05.01010128056.351
Sertraline4202200.293.425260

Im sure you'll enjoy the PRC compounds alot more than Venlafaxine! =D

(gamma) γ-amino alcohol compounds such as those currently being persued by Paul R. Carlier and Elliott Richelson.[1][2][3][4].
These are antidepressants that are stronger than Venlafaxine[1990].[5]

Indatraline

Triple Mode Pat Retrieval

Miscellaneous

References

  1. ^ [1]European Journal of Pharmacology Volume 555, Issue 1 , 19 January 2007, Pages 30-36
  2. ^ United States Patent 6,700,018 Richelson, et al. March 2, 2004
  3. ^ United States Patent 6,069,177 Carlier, et al. May 30, 2000
  4. ^ [2] Bioorganic & Medicinal Chemistry Letters, V8, Issue 5 , 1998, pp 487-492
  5. ^ [3]J. Med. Chem.; 1990; 33(10); 2899-2905.

External links

Template:ChemicalSources Behavioural despair test