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Biogenic Amine Transport Inhibitors

Mechanism of Action of Selective Monoaminergic Reuptake Inhibitors. During neurotransmission, monoamine neurotransmitters such as serotonin, dopamine or norepinephrine, are released into the synaptic cleft from storage vesicles present in the pre-synaptic neuron (A). The neurotransmitters then bind to their respective receptors on the post-synaptic neuron, thereby transferring the signal. The actions of the neurotransmitters are terminated via their reuptake into the pre-synaptic neuron via specific transporter proteins following which the neurotransmitter is taken up into the vesicles for re-release. When a monoaminergic reuptake inhibitor is present (B), it binds to the monoamine transporter and blocks the reuptake of the neurotransmitter whose levels increase in the synaptic cleft thereby enhancing neurotransmission.

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Image	Description	Biochem/physiol Actions	CAS Number	Product #
	(−)-2β-Carbomethoxy-3β-(4-iodophenyl)nortropane crystalline	5-HT serotonin transporter inhibitor; precursor of [¹²³I]nor-β-CIT, a radioligand for SPECT imaging of the 5-HT transporter.	136794-87-1	C155
	(R)-Tomoxetine hydrochloride solid	Norepinephrine uptake blocker.	82248-59-7	T7947
	6-Nitroquipazine maleate salt solid	Potent and selective serotonin transport blocker.	77372-73-7	Q109
	Alaproclate hydrochloride	Potent and selective serotonin uptake inhibitor.	60719-83-7	A164
	Amitriptyline hydrochloride ≥98% (TLC), powder	Tricyclic antidepressant; inhibits the norepinephrine and serotonin transporters with K_is of 100 nM and 14.7 nM, respectively; high in vitro affinity for α₁-adrenoceptors, serotonin and muscarinic acetylcholine receptors.	549-18-8	A8404
	Amoxapine	Tricyclic antidepressant; inhibits uptake of norepinephrine; inhibits 5-HT₂ serotonergic receptors.	14028-44-5	A129
	BTCP hydrochloride solid	Potent and selective blocker of dopamine transport with little affinity for phencyclidine sites.	112726-66-6	B138
	Bupropion hydrochloride ≥98% (HPLC), solid	Inhibits the dopamine and norepinephrine transporters with K_is of 2.8 μM and 1.4 μM, respectively. Does not inhibit the serotonin transporter (K_i = 45 μM). Antidepressant.	31677-93-7	B102
	Citalopram hydrobromide solid	Potent and selective serotonin uptake inhibitor (K_i = 5.4 nM); antidepressant	59729-32-7	C7861
	Clomipramine hydrochloride ≥98% (HPLC), powder	Tricyclic antidepressant; inhibits serotonin and norepinephrine transporters.	17321-77-6	C7291
	Desipramine hydrochloride ≥98% (TLC), powder	Tricyclic antidepressant that is a more potent inhibitor of the norepinephrine transporter (K_i = 4 nM) than the serotonin transporter (K_i = 61 nM).	58-28-6	D3900
	Desvenlafaxine hydrochloride ≥98% (HPLC), solid	Desvenlafaxine hydrochloride is a dual SERT/NET reuptake inhibitor. It is a major active metabolite of venlafaxine (#542); brain penetrant; K_i = 40 nM and 122 nM for hSERT and hNET, respectively (weak binding at the hDAT). Inhibition of [3H]5-HT or [3H]NE uptake for the hSERT or hNET produced IC₅₀ values of 47 and 531 nM.	300827-87-6	D2069
	Doxepin hydrochloride ~85% E-isomer basis, ≥98% (GC), 15% Z-isomer basis, powder	Tricyclic antidepressant that is a more potent inhibitor of norepinephrine uptake than of serotonin uptake; antagonist at H₁ histamine, muscarinic cholinergic, and α-adrenoreceptors.	1229-29-4	D4526
	Fluoxetine hydrochloride solid	Selective serotonin reuptake inhibitor; antidepressant.	56296-78-7	F132
	Fluvoxamine maleate solid	Selective serotonin reuptake inhibitor; antidepressant.	61718-82-9	F2802
	GBR 12909 dihydrochloride solid, ≥98% (HPLC)	Highly selective dopamine reuptake inhibitor with behavioral effects similar to cocaine.	67469-78-7	D052
	GBR 12935 dihydrochloride ≥98% (TLC), powder	Inhibits the dopamine and norepinephrine transporters with K_is of 21.5 nM and 225 nM, respectively. Does not inhibit the serotonin transporter (K_i = 6.5 μM). Binds to a nondopaminergic piperazine site in blood platelets and brain that has been identified as cytochrome P450.	67469-81-2	G9659
	GYKI 52895 solid	Selective dopamine uptake inhibitor; antiparkinsonian; antidepressant.		G120
	Imipramine hydrochloride ≥99% (TLC), crystalline	Tricyclic antidepressant; inhibits the serotonin and norepinephrine transporters with K_is of 7.7 nM and 67 nM, respectively. Has little effect on the dopamine transporter (K_i = 25 μM).	113-52-0	I7379
	Indatraline hydrochloride solid	Potent inhibitor of dopamine, norepinephrine and serotonin uptake.	96850-13-4	I119
	Lofepramine hydrochloride ≥98% (HPLC), solid	Lofepramine is an antidepressant; serotonin and norepinephrine re-uptake inhibitor (SNRI).	26786-32-3	L8792
	Maprotiline hydrochloride >99% (HPLC), powder	Selective norepinephrine uptake inhibitor.	10347-81-6	M9651
	Mazindol ≥98% (TLC), powder	Anorectic agent; inhibits the dopamine, norepinephrine and serotonin transporters with K_is of 27.6 nM, 3.2 nM, and 153 nM, respectively.	22232-71-9	M2017
	Mirtazapine ≥98% (HPLC), solid	Mirtazapine is a noradrenergic and specific serotonergic antidepressant (NaSSA). Mirtazapineant agonizes selective adrenergic and serotonergic receptors so that both NE release and 5-HT_1A mediated serotonergic signaling are increased.	61337-67-5	M0443
	Nefazodone hydrochloride ≥98% (HPLC), solid	Novel antidepressant; mixed 5-HT_2A serotonin receptor antagonist/serotonin uptake inhibitor.	82752-99-6	N5536
	Nisoxetine hydrochloride solid, ≥98% (HPLC)	Potent and selective inhibitor of the norepinephrine transporter (K_i = 5.1 nM).	57754-86-6	N151
	Nomifensine maleate salt	Selective dopamine uptake inhibitor interacting with the dopamine transporter at a site different from that of cocaine; antidepressant.	32795-47-4	N1530
	Norfluoxetine hydrochloride ≥97%, solid	Fluoxetine metabolite; more potent inhibitor of serotonin uptake than fluoxetine with a half-life in vivo of 5-7 days.	83891-03-6	F133
	Nortriptyline hydrochloride ≥98% (TLC), powder	Tricyclic antidepressant that is a more potent inhibitor of the norepinephrine transporter (K_i = 3.4 nM) than the serotonin transporter (K_i = 161 nM). 5-HT₂ serotonin receptor antagonist.	894-71-3	N7261
	Paroxetine hydrochloride hemihydrate ≥98% (HPLC), solid	Paroxetine hydrochloride hemihydrate is one of the most potent and selective of the selective serotonin reuptake inhibitors (SSRI); antidepressant	110429-35-1	P9623
	Protriptyline hydrochloride ≥98% (TLC), powder	Norepinephrine uptake blocker.	1225-55-4	P8813
	R-(−)-Fluoxetine hydrochloride >98% (HPLC), solid	Selective serotonin reuptake inhibitor.	114247-09-5	F1678
	Reboxetine mesylate hydrate >96% (HPLC), solid	Reboxetine mesylate hydrate is a selective noradrenaline uptake inhibitor.	98769-84-7 (anhydrous)	R6527
	S-(+)-Fluoxetine hydrochloride ≥98% (HPLC), solid	Selective serotonin reuptake inhibitor.	114247-06-2	F1553
	Sibutramine hydrochloride monohydrate ≥98% (HPLC), solid	Sibutramine is a serotonin and noradrenaline reuptake inhibitor (SNRI). It is an antiobesity drug, which decreases calorie intake and increases energy expanditure. Sibutramine antagonizes MPTP-induced dopamine depletion in mouse brain.	125494-59-9	S9944
	Tianeptine sodium salt solid	Tricyclic antidepressant; enhances serotonin uptake.	30123-17-2	T1692
	Trazodone hydrochloride >99% (HPLC), powder	Antidepressant that potentiates the activity of serotonin uptake blockers and has full 5-HT_2C serotonin receptor agonist activity. It is metabolized to the 5-HT₁ serotonin receptor agonist 1-(3-Chlorophenyl)piperazine.	25332-39-2	T6154
	Trimipramine maleate salt ≥98% (TLC), powder	Antidepressant; serotonin transport blocker that also blocks norepinephrine uptake.	521-78-8	T3146
	Venlafaxine hydrochloride ≥98% (HPLC), powder	Venlafaxine is an antidepressant. The mechanism of the antidepresant action of venlafaxine in humans is associated with its potentiation of neurotransmitter activity in the CNS. Venlafaxine is a potent inhibitor of neuronal serotonin and norepinephrine reuptake and weak inhibitor of dopamine reuptake. Venlafaxine has no significant activity for muscarinic, histaminergic, or α-1 adrenergic receptors in vitro. Venlafaxine does not possess MAO inhibitor activity.	99300-78-4	V7264
	Zimelidine dihydrochloride solid	Serotonin transport blocker; antidepressant.	61129-30-4	Z101
	β-CFT naphthalenedisulfonate monohydrate solid	Cocaine analog that inhibits the dopamine, norepinephrine, and serotonin transporters with K_is of 26.1 nM, 31.9 nM, and 127 nM, respectively. [¹¹C]-β-CFT and [¹⁸F]-β-CFT are ligands for PET imaging of the dopamine transporter in vivo.	77210-32-3 (anhydrous)	C124

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