Paroxetine HCl 78246-49-8

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Molecular Weight: 365.83 Paroxetine HCl is an antidepressant drug of the SSRI type.


Paroxetine apparently exerts their antidepressant activity by increasing
the concentration of 5-HT in the extracellular compartment, thereby
enhancing serotoninergic neurotransmission. Paroxetine (1-300 μM)
results in a concentration-dependent reduction in the firing rate of DRN
serotoninergic neurons with IC50 values of 1.4 μM in the ACSF
superfusing brain stem slices. Paroxetine is a highly
Potent Inhibitor of desipramine hydroxylation, the inhibition constant
(Ki) value of 2.0 mM indicated greater inhibiting potency than
fluoxetine or norfluoxetine.


Paroxetine is shown to be a
potent (Ki = 1.1 nM) and specific inhibitor of [3H]-5-hydroxytryptamine
(5-HT) uptake into rat cortical and hypothalamic synaptosomes in vitro.
Paroxetine demonstrates weak affinity for muscarinic receptors (Ki = 89
nM) but is at least 15 fold weaker than amitriptyline (Ki = 5.1 nM). Paroxetine inactivates CYP2D6 via the formation of a metabolite intermediate complex.


Paroxetine produces a dose-related inhibition of [3H]-5-HT uptake (ED50 =
1.9 mg/kg) into rat hypothalamic synaptosomes ex vivo with little
effect on [3H]-l-noradrenaline (NA) uptake (ED50 greater than 30 mg/kg).
Paroxetine (ED50 1-3 mg/kg PO) prevents the 5-HT depleting effect of
p-chloroamphetamine (PCA) in rat brain, demonstrating 5-HT uptake
blockade in vivo.





Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	365.83
Formula	C19H20FNO3.HCl
CAS No.	78246-49-8

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	73 mg/mL (199.54 mM)
		Water	10 mg/mL (27.33 mM)
		Ethanol	35 mg/mL (95.67 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	(3S,4R)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)-piperidine, hydrochloride (1:1)

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