orphenadrine citrate

[Description]:

Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.Target: NMDA ReceptorOrphenadrine has been used as an antiparkinsonian, antispastic and analgesic drug. Orphenadrine inhibits [3H]MK-801 binding to the phencyclidine (PCP) binding site of the N-methyl-D-aspartate (NMDA)-receptor in homogenates of postmortem human frontal cortex with a Ki-value of 6.0 +/- 0.7 microM. The NMDA receptor antagonistic effects of orphenadrine were assessed using concentration- and patch-clamp techniques on cultured superior colliculus neurones. Orphenadrine blocked open NMDA receptor channels with fast kinetics and in a strongly voltage-dependent manner. The IC50-value against steady state currents at -70 mV was 16.2 +/- 1.6 microM (n = 6). Orphenadrine exhibited relatively fast, concentration-dependent open channel blocking kinetics (Kon 0.013 +/- 0.002 10(6) M-1S-1) whereas the offset rate was concentration-independent (Koff 0.230 +/- 0.004 S-1) [1]. Orphenadrine competitively inhibited [3H]nisoxetine binding in rat vas deferens membranes (Ki = 1.05+/-0.20 microM). It can be concluded that orphenadrine, at low micromolar concentrations, interacts with the noradrenaline reuptake system inhibiting its functionality and thus potentiating the effect of noradrenaline [2].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

[References]

[1]. Kornhuber, J., et al., Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies. J Neural Transm Gen Sect, 1995. 102(3): p. 237-46.

[2]. Pubill, D., et al., Assessment of the adrenergic effects of orphenadrine in rat vas deferens. J Pharm Pharmacol, 1999. 51(3): p. 307-12.

[Related Small Molecules]

[ Density]:
1.014 g/cm3

[ Boiling Point ]:
363ºC at 760 mmHg

[ Melting Point ]:
132-134ºC

[ Molecular Formula ]:
C₂₄H₃₁NO₈

[ Molecular Weight ]:
461.50500

[ Flash Point ]:
107.1ºC

[ Exact Mass ]:
461.20500

[ PSA ]:
133.60000

[ LogP ]:
2.75980

[ Storage condition ]:
2-8°C

Click to get detail MSDS

[ Symbol ]:

GHS07, GHS08

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H351

[ Precautionary Statements ]:
P281

[ Hazard Codes ]:
Xi:Irritant;

[ Risk Phrases ]:
R22;R40

[ Safety Phrases ]:
S22-S36

[ RIDADR ]:
UN 3249

[ WGK Germany ]:
3

[ Packaging Group ]:
III

[ Hazard Class ]:
6.1(b)

Preclinical evaluation of marketed sodium channel blockers in a rat model of myotonia discloses promising antimyotonic drugs.

Exp. Neurol. 255 , 96-102, (2014)

Although the sodium channel blocker mexiletine is considered the first-line drug in myotonia, some patients experiment adverse effects, while others do not gain any benefit. Other antimyotonic drugs a...

Spectrophotometric determination of tizanidine and orphenadrine via ion pair complex formation using eosin Y.

Chem. Cent. J. 5 , 60, (2011)

A simple, sensitive and rapid spectrophotometric method was developed and validated for the determination of two skeletal muscle relaxants namely, tizanidine hydrochloride (I) and orphenadrine citrate...

Reduction of tinnitus severity by the centrally acting muscle relaxant cyclobenzaprine: an open-label pilot study.

Audiol. Neurootol. 17(3) , 179-88, (2012)

Tinnitus, the phantom perception of sounds, is a highly prevalent disorder. Although a wide variety of drugs have been investigated off label for the treatment of tinnitus, there is no approved pharma...

Names

Biological Activity

Chemical & Physical Properties

MSDS

Click to get detail MSDS

Safety Information

Articles

Related Compounds