orphenadrine citrate
orphenadrine citrate structure
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Common Name | orphenadrine citrate | ||
|---|---|---|---|---|
| CAS Number | 4682-36-4 | Molecular Weight | 461.50500 | |
| Density | 1.014 g/cm3 | Boiling Point | 363ºC at 760 mmHg | |
| Molecular Formula | C24H31NO8 | Melting Point | 132-134ºC | |
| MSDS | Chinese USA | Flash Point | 107.1ºC | |
| Symbol |
GHS07, GHS08 |
Signal Word | Warning | |
Use of orphenadrine citrateOrphenadrine 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]. |
This table lists Chinese names, IUPAC names and various aliases of this chemical substance.
| Name | orphenadrine citrate |
|---|---|
| Synonym | More Synonyms |
This table contains bioactivity, target information and biological‑assay experimental data of this compound.
| 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]. |
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| Related Catalog | |
| References |
This table shows physicochemical parameters including melting point, boiling point, density, solubility and optical rotation. Missing data is marked as N/A.
| 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 |
| InChIKey | MMMNTDFSPSQXJP-UHFFFAOYSA-N |
| SMILES | Cc1ccccc1C(OCCN(C)C)c1ccccc1.O=C(O)CC(O)(CC(=O)O)C(=O)O |
| Storage condition | 2-8°C |
This table provides MSDS information including hazard classification, first‑aid, fire‑fighting, spill handling, operation and storage instructions.
This table covers safety warnings, protective measures, incompatible substances and disposal guidelines for this compound.
| 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) |
This table lists relevant public references with title, journal and publication metadata for this compound.
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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... |
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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... |
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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... |
This table collects all English aliases, systematic names and CAS‑related synonyms of the compound.
| Orphenadrine Citrate |
| Orphenadrine Citrate Salt |
| MFCD00079197 |
| EINECS 225-137-5 |
This section contains frequently‑asked‑questions about this compound, including basic parameters, properties, storage conditions and corresponding answers.
| Q: What is the molecular weight of orphenadrine citrate? |
| A: Molecular weight of orphenadrine citrate is 461.50500. |
| Q: What English synonyms does orphenadrine citrate have? |
| A: English synonyms of orphenadrine citrate: Orphenadrine Citrate, Orphenadrine Citrate Salt, MFCD00079197, EINECS 225-137-5. |
| Q: What is the LogP of orphenadrine citrate? |
| A: LogP of orphenadrine citrate is 2.75980. |
| Q: What are the storage conditions for orphenadrine citrate? |
| A: Storage conditions for orphenadrine citrate: 2-8°C. |
| Q: What is the molecular formula of orphenadrine citrate? |
| A: Molecular formula of orphenadrine citrate is C24H31NO8. |
| Q: What is the safety information for orphenadrine citrate? |
| A: Safety information for orphenadrine citrate: S22-S36. |
| Q: What is the InChIKey of orphenadrine citrate? |
| A: InChIKey of orphenadrine citrate is MMMNTDFSPSQXJP-UHFFFAOYSA-N. |
| Q: What is the melting point of orphenadrine citrate? |
| A: Melting point of orphenadrine citrate is 132-134ºC. |
| Q: What is the English name of orphenadrine citrate? |
| A: The English name of orphenadrine citrate is orphenadrine citrate. |
| Q: What is the polar surface area (PSA) of orphenadrine citrate? |
| A: Polar surface area (PSA) of orphenadrine citrate is 133.60000. |
This table lists manufacturers and suppliers of this compound, including vendor names and product supply reference information.
| Shanghai Nianxing Industrial Co., Ltd |
| Dayang Chem (Hangzhou) Co., Ltd. |
| Henan Tianfu Chemical Co., Ltd. |