83-98-7
Chemical Structure
Orphenadrine
Synonym(s): (±)-Orphenadrine
- CAS No.: 83-98-7
- Formula:C18H23NO
- Molecular Weight:269.38
InChIKey: QVYRGXJJSLMXQH-UHFFFAOYSA-N
SMILES: CN(C)CCOC(C1=C(C)C=CC=C1)C2=CC=CC=C2
Biological Activity: Orphenadrine ((±)-Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of [3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and CYP2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Orphenadrine | 99.71% | Orphenadrine ((±)-Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of [3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and CYP2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation. | ||||||||||||||||||||
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Orphenadrine-d3 | Orphenadrine-d3 is the deuterium labeled Orphenadrine. | |||||||||||||||||||||
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Toladryl | 97.23% | Toladryl is a derivative of Diphenhydramine (HY-B0303), capable of penetrating the blood-brain barrier and possessing oral activity, as well as antihistamine and anticholinergic activities. The anticholinergic activity of Toladryl is approximately one-tenth that of Diphenhydramine (HY-B0303), and its protective effect against lethal doses of histamine in guinea pigs is 2 to 4 times that of Diphenhydramine (HY-B0303). The side effects of Toladryl are fewer and milder than those of Diphenhydramine (HY-B0303), but at higher doses, it may cause central nervous system symptoms such as insomnia, agitation, and disorientation. Toladryl can be used for research in allergic diseases. | ||||||||||||||||||||
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Diphenhydramine hydrochloride (Standard) | 99.90% | Diphenhydramine (hydrochloride) (Standard) is the analytical standard of Diphenhydramine (hydrochloride). This product is intended for research and analytical applications. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB). | ||||||||||||||||||||
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Diphenhydramine (Standard) | 98.69% | Diphenhydramine (Standard) is the analytical standard of Diphenhydramine. This product is intended for research and analytical applications. Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) . | ||||||||||||||||||||
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Diphenhydramine-d3 | Diphenhydramine-d3 is the deuterium labeled Diphenhydramine (HY-B0303). Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB). | |||||||||||||||||||||
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Orphenadrine hydrochloride (Standard) | ≥98% | Orphenadrine (hydrochloride) (Standard) is the analytical standard of Orphenadrine (hydrochloride). This product is intended for research and analytical applications. Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases. | ||||||||||||||||||||
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Orphenadrine-d3 hydrochloride | Orphenadrine-d3 (hydrochloride) is the deuterium labeled Orphenadrine hydrochloride. Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases. | |||||||||||||||||||||
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Bromodiphenhydramine | Bromodiphenhydramine (Ambodryl) is a potent antihistamine with antimicrobial property. Bromodiphenhydramine inhibits a large number of Gram negative and Gram positive bacteria. Bromodiphenhydramine can be used for cutaneous allergies research. | |||||||||||||||||||||
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Bromodiphenhydramine hydrochloride | 97.34% | Bromodiphenhydramine hydrochloride is a potent antihistamine with antimicrobial property. Bromodiphenhydramine hydrochloride inhibits a large number of Gram negative and Gram positive bacteria. Bromodiphenhydramine hydrochloride can be used for cutaneous allergies research. | ||||||||||||||||||||
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2-(Benzhydryloxy)-N-methylethan-1-amine hydrochloride (Standard) | 99.83% | 2-(Benzhydryloxy)-N-methylethan-1-amine hydrochloride (Standard) is the analytical standard of 2-(Benzhydryloxy)-N-methylethan-1-amine hydrochloride. This product is intended for research and analytical applications. | ||||||||||||||||||||
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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):237-46. [Content Brief]
- [2]. Morita R, et al. Liver tumor promoting effect of orphenadrine in rats and its possible mechanism of action including CAR activation and oxidative stress. J Toxicol Sci. 2013;38(3):403-13. [Content Brief]
- [3]. Pubill D, et al. Orphenadrine prevents 3-nitropropionic acid-induced neurotoxicity in vitro and in vivo. Br J Pharmacol. 2001 Feb;132(3):693-702. [Content Brief]