Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group.

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Carlier PR, Lo MM, Lo PC, Richelson E, Tatsumi M, Reynolds IJ, Sharma TA

Bioorg Med Chem Lett. 1998 Mar 3;8(5):487-92.

PubMed ID

9871604 [ View in PubMed

]

Abstract

A series of gamma-amino alcohols were synthesized and screened for reuptake inhibition and noncompetitive NMDA antagonism. Compound (+/-)-3f simultaneously and potently inhibits reuptake of 5-HT, NE, and DA, representing a potential wide-spectrum reuptake inhibitor antidepressant. In addition, comparative rat and human studies uncovered a species-selective DA reuptake inhibitor (+/-)-2e, KD(hDAT)/KD(rDAT) = 97.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Atomoxetine	Sodium-dependent noradrenaline transporter	Kd (nM)	2.03	N/A	N/A	Details
Atomoxetine	Sodium-dependent serotonin transporter	Kd (nM)	8.9	N/A	N/A	Details
Fluoxetine	Sodium-dependent serotonin transporter	Kd (nM)	0.81	N/A	N/A	Details
Nefazodone	Sodium-dependent dopamine transporter	Kd (nM)	360	N/A	N/A	Details
Nefazodone	Sodium-dependent noradrenaline transporter	Kd (nM)	360	N/A	N/A	Details
Nefazodone	Sodium-dependent serotonin transporter	Kd (nM)	200	N/A	N/A	Details
Paroxetine	Sodium-dependent noradrenaline transporter	Kd (nM)	40	N/A	N/A	Details
Paroxetine	Sodium-dependent serotonin transporter	Kd (nM)	0.13	N/A	N/A	Details
Sertraline	Sodium-dependent dopamine transporter	Kd (nM)	25	N/A	N/A	Details
Sertraline	Sodium-dependent serotonin transporter	Kd (nM)	0.29	N/A	N/A	Details
Venlafaxine	Sodium-dependent dopamine transporter	Kd (nM)	9300	N/A	N/A	Details
Venlafaxine	Sodium-dependent noradrenaline transporter	Kd (nM)	1060	N/A	N/A	Details
Venlafaxine	Sodium-dependent serotonin transporter	Kd (nM)	8.9	N/A	N/A	Details