quinupramine

Names

[ Name ]:
quinupramine

[Synonym ]:
Quinupraminum
Kinupril
Kevopril
Quinupramina
Quinupramine

Biological Activity

[Description]:

Quinupramine is an orally active antidepressant. Quinupramine can penetrate into the CNS and affect some of the processes of neurotransmission. The antidepressant activity of quinupramine is associated with the central serotonin system, but not with the β-adrenergic system[1][2].

[Related Catalog]:

Research Areas >> Neurological Disease

[In Vivo]

Quinupramine (10 mg/kg, PO, twice daily for 10 days) causes a down-regulation of serotonin S2 receptors in the frontal cortex of the rat[2]. Quinupramine-EVA matrix containing a permeation enhancer can be a good transdermal delivery system for providing sustained plasma concentrations[3]. Animal Model: Sprague-Dawley rats (Male, 220-270 g) Dosage: 10 mg/kg Administration: PO, twice daily for 10 days Result: Caused a down-requlation of serotonin S2 receptors in the frontal cortex of the rat, did not alter the binding populations of Q-adrenergic, muscarinic cholinergic and a2-adrenergic receptors in the rat brain.

[References]

[1]. [1] Sakamoto H, et al. Effects of quinupramine on the central monoamine uptake systems and involvement of pharmacokinetics in its pharmacological activities. Jpn J Pharmacol. 1987;45(2):169-175.

[2]. [2] Sakamoto H, et al. Down-regulation of central serotonin S2 receptors after repeated treatment with quinupramine in rats. Jpn J Pharmacol. 1987;43(4):369-377.

[3]. [3] Shin SC, et al. Development and biopharmaceutical evaluation of quinupramine-EVA matrix containing penetration enhancer for the enhanced transdermal absorption in rats. Pharm Dev Technol. 2007;12(5):429-436.

Chemical & Physical Properties

[ Density]:
1.19g/cm3

[ Boiling Point ]:
445.2ºC at 760mmHg

[ Molecular Formula ]:
C₂₁H₂₄N₂

[ Molecular Weight ]:
304.43

[ Flash Point ]:
201.7ºC

[ Exact Mass ]:
304.19400

[ PSA ]:
6.48000

[ LogP ]:
4.02040

[ Index of Refraction ]:
1.667

Safety Information

[ RIDADR ]:
UN 3249

[ Packaging Group ]:
III

[ Hazard Class ]:
6.1(b)

[ HS Code ]:
2933990090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%