Serotonin–norepinephrine–dopamine reuptake inhibitor: Difference between revisions
mNo edit summary |
|||
Line 1: | Line 1: | ||
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)
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)
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.
- PRC50 is species selective, it behaves differently in rats to humans, wrt DAT.
Compound | hNAT Kd (nM) | hNAT Ki (nM) | hSERT Kd (nM) | hSERT Ki (nM) | hDAT Kd (nM) | hDAT Ki (nM) |
---|---|---|---|---|---|---|
PRC050 | 0.40 | 1.2 | 6.0 | 12 | 120 | 43 |
PRC025 | 19 | 10 | 6.0 | 6.0 | 100 | 53 |
Venlafaxine | 1060 | 210 | 9.0 | 39 | 9300 | 5300 |
Paroxetine | 40 | 33 | 0.13 | 0.73 | 490 | 1700 |
Imipramine | 37 | 14 | 1.4 | 41 | 8500 | 11000 |
Nomifensine | 16.0 | 5.0 | 1010 | 1280 | 56.3 | 51 |
Sertraline | 420 | 220 | 0.29 | 3.4 | 25 | 260 |
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]European Journal of Pharmacology Volume 555, Issue 1 , 19 January 2007, Pages 30-36
- ^ United States Patent 6,700,018 Richelson, et al. March 2, 2004
- ^ United States Patent 6,069,177 Carlier, et al. May 30, 2000
- ^ [2] Bioorganic & Medicinal Chemistry Letters, V8, Issue 5 , 1998, pp 487-492
- ^ [3]J. Med. Chem.; 1990; 33(10); 2899-2905.