Page last updated: 2024-12-05

eperisone

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Description

Eperisone is a centrally acting muscle relaxant with a complex mechanism of action. It is thought to act by inhibiting the release of excitatory neurotransmitters, such as glutamate and acetylcholine, from nerve terminals. Eperisone also has antioxidant and anti-inflammatory properties. Eperisone is primarily used to treat muscle spasms, stiffness, and pain associated with musculoskeletal disorders, such as spinal stenosis, cervical spondylosis, and lumbar disc herniation. Eperisone is studied for its potential to improve motor function and reduce spasticity in patients with conditions such as spinal cord injury, stroke, and cerebral palsy. Eperisone is generally well-tolerated, but common side effects may include dizziness, drowsiness, nausea, and dry mouth. It is important to note that eperisone may interact with other medications, so it is essential to consult with a healthcare professional before taking it.'

eperisone : A racemate that is an equimolar mixture of (R)- and (S)-eperisone. It is used (as the hydrochloride salt) as a muscle relaxant for the symptomatic treatment of muscle spasm and spasticity. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

1-(4-ethylphenyl)-2-methyl-3-(piperidin-1-yl)propan-1-one : An aromatic ketone that is N-propylpiperidine in which a hydrogen at positon 2 of the propyl group is replaced by a p-ethylbenzoyl group. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID3236
CHEMBL ID1902981
CHEBI ID77070
SCHEMBL ID194769
MeSH IDM0097328
PubMed CID123698
CHEMBL ID2360601
CHEBI ID31540
SCHEMBL ID218337
MeSH IDM0097328

Synonyms (90)

Synonym
AC-12144
eperisone [inn]
eperisone
brn 1246496
4'-ethyl-2-methyl-3-piperidinopropiophenone
eperisona [inn-spanish]
c17h25no
(+-)-eperisone
1-(4-ethylphenyl)-2-methyl-3-(1-piperidinyl)-1-propanone
eperisonum [inn-latin]
1-propanone, 1-(4-ethylphenyl)-2-methyl-3-(1-piperidinyl)-
1-(4-ethylphenyl)-2-methyl-3-(piperidin-1-yl)propan-1-one
64840-90-0
D07898
eperisone (inn)
1-(4-ethylphenyl)-2-methyl-3-piperidin-1-ylpropan-1-one
AKOS015960753
eperisona
2m2p0551d3 ,
unii-2m2p0551d3
eperisonum
chebi:77070 ,
CHEMBL1902981
FT-0630750
eperisone [jan]
eperisone [mi]
eperisone [who-dd]
SCHEMBL194769
DTXSID5040671
DB08992
(2rs)-1-(4-ethylphenyl)-2-methyl-3-(1-piperidyl)propan-1-one
HY-128891
Q426401
BRD-A04252265-001-01-8
CS-0101898
AC-15896
AKOS015843965
e-2000 ,
empp
eperisone hydrochloride
myonal
4'-ethyl-2-methyl-3-piperidinopropiophenone hydrochloride
e-646
e 0646
1-propanone, 1-(4-ethylphenyl)-2-methyl-3-(1-piperidinyl)-, hydrochloride
mional
(4'-ethyl-2-methyl-3-piperidino)propiophenone
propiophenone, 4'-ethyl-2-methyl-3-piperidino-, hydrochloride
eperisone hydrochloride (jp17)
56839-43-1
epenard (tn)
D01671
NCGC00167973-01
A831198
1-(4-ethylphenyl)-2-methyl-3-(1-piperidyl)propan-1-one hydrochloride;eperisone hcl
eperisone hcl
tox21_112599
dtxsid8047844 ,
dtxcid8027822
cas-56839-43-1
u38o8u7p6x ,
unii-u38o8u7p6x
eperisone hydrochloride [jan]
dw-1030
FT-0602324
1-(4-ethylphenyl)-2-methyl-3-(1-piperidinyl)-1-propanone hydrochloride
eperisone hydrochloride [mart.]
eperisone hydrochloride [mi]
eperisone hydrochloride [who-dd]
SCHEMBL218337
GTAXGNCCEYZRII-UHFFFAOYSA-N
e2000
NCGC00167973-02
tox21_112599_1
KS-5241
CHEMBL2360601
CHEBI:31540
1-(4-ethylphenyl)-2-methyl-3-(piperidin-1-yl)propan-1-one hydrochloride
HY-B1901
Q27889924
mfcd00941459
BCP11969
1-(4-ethylphenyl)-2-methyl-3-(piperidin-1-yl)propan-1-onehydrochloride
eperisone, hcl
CCG-267425
CS-0013960
1-(4-ethylphenyl)-2-methyl-3-piperidin-1-ylpropan-1-one;hydrochloride
D95097
S4877
eperisonehydrochloride

Research Excerpts

Overview

Eperisone hydrochloride is a centrally acting muscle relaxant prescribed for muscle stiffness. It acts by depressing the activities of α and γ efferent neurons in the spinal cord and supraspinal structures. It is an analgesic and antispastic drug used for spastic diseases.

ExcerptReferenceRelevance
"Eperisone is a commonly prescribed oral muscle relaxant, but few studies have been conducted of eperisone-induced hypersensitivity reactions."( Clinical characteristics of eperisone-induced immediate-type hypersensitivity.
An, J; Cho, YS; Kang, Y; Kim, TB; Kwon, HS; Lee, JH; Moon, HB; Shin, B; Song, WJ; Won, HK; Yoon, SY, 2020
)
2.29
"Eperisone hydrochloride is a centrally acting muscle relaxant prescribed for muscle stiffness that acts by depressing the activities of α and γ efferent neurons in the spinal cord and supraspinal structures. "( Serum concentration of eperisone hydrochloride correlates with QT interval.
Amino, M; Inokuchi, S; Miura, N; Morita, S; Saito, T; Yamagiwa, T, 2014
)
2.16
"Eperisone hydrochloride is an analgesic and antispastic drug used for spastic diseases such as spastic paralysis in cerebrovascular diseases, cervical spondylosis, and periarthritis."( Eperisone hydrochloride-induced maculopapular rash.
Balaraddiyavar, N; Bhushan, A; Huggi, G; Kotinatot, BC,
)
2.3
"Eperisone hydrochloride is a centrally acting muscle relaxant that performs by blocking calcium channels."( Pharmacokinetic Interactions Between Pelubiprofen and Eperisone Hydrochloride: A Randomized, Open-label, Crossover Study of Healthy Korean Men.
Chung, EK; Kim, HS; Kim, JI; Lee, KT; Noh, GJ; Ryu, JH, 2017
)
1.42
"Eperisone is a centrally acting muscle relaxant widely used for the therapeutic treatment of spastic patients to relieve muscle stiffness and back pain. "( Characterization of human cytochrome P450 enzymes involved in the biotransformation of eperisone.
Jin, C; Kim, DH; Kim, NS; Lee, J; Sohn, DR; Yoo, HH, 2009
)
2.02
"Eperisone is a central muscle relaxant used in several conditions, but its therapeutic potential in spastic palsy needs to be verified."( Efficacy and tolerability of eperisone in patients with spastic palsy: a cross-over, placebo-controlled dose-ranging trial.
Bresolin, N; Pecori, A; Zucca, C,
)
1.14
"Eperisone hydrochloride is a centrally acting muscle relaxant, and triazolam is a short-acting benzodiazepine. "( A case of torsades de pointes induced by severe QT prolongation after an overdose of eperisone and triazolam in a patient receiving nifedipine.
Amino, M; Inokuchi, S; Morita, S; Saito, T; Yamagiwa, T; Yamamoto, R, 2010
)
2.03
"As eperisone is a racemic compound with one chiral centre, the carbonyl reduced metabolite of eperisone (M5) may have four possible diastereoisomeric structures."( Enantioselective carbonyl reduction of eperisone in human liver microsomes.
Kim, DH; Kim, MJ; Kim, NS; Shin, D; Shin, JG; Yoo, HH, 2011
)
1.15
"Eperisone hydrochloride is a centrally acting muscle relaxant inhibiting the pain reflex pathway, having a vasodilator effect."( Evaluation of eperisone hydrochloride in the treatment of acute musculoskeletal spasm associated with low back pain: a randomized, double-blind, placebo-controlled trial.
Chandanwale, AS; Chopra, A; Gaikwad, S; Goregaonkar, A; Langade, DG; Maroli, S; Medhi, B; Mehta, SC; Naikwadi, A; Pawar, DR; Shah, V,
)
1.93

Effects

Eperisone hydrochloride has been recently proposed as a muscle relaxant for the treatment of muscle contracture and chronic low back pain. It is devoid of clinically relevant sedative effects on the central nervous system (CNS)

ExcerptReferenceRelevance
"Eperisone has a sympatho-suppressive action in resting skeletal muscles, but has no effect on MSA in actively contracting muscles, e.g."( Effect of a centrally-acting muscle relaxant, eperisone hydrochloride, on muscle sympathetic nerve activity in humans.
Ishida, G; Iwase, S; Mano, T; Saito, M,
)
1.11
"Eperisone hydrochloride has been recently proposed as a muscle relaxant for the treatment of muscle contracture and chronic low back pain (LBP) as it is devoid of clinically relevant sedative effects on the central nervous system (CNS). "( Open experience with a new myorelaxant agent for low back pain.
Guerra, L; Sartini, S, 2008
)
1.79
"Eperisone has a sympatho-suppressive action in resting skeletal muscles, but has no effect on MSA in actively contracting muscles, e.g."( Effect of a centrally-acting muscle relaxant, eperisone hydrochloride, on muscle sympathetic nerve activity in humans.
Ishida, G; Iwase, S; Mano, T; Saito, M,
)
1.11

Treatment

ExcerptReferenceRelevance
"Treatment with eperisone attenuated the contractions induced by norepinephrine and serotonin in the arteries and those by clonidine and phenylephrine in the veins."( Mechanisms of action of eperisone on isolated dog saphenous arteries and veins.
Bian, K; Inoue, S; Okamura, T; Okunishi, H; Toda, N, 1989
)
0.92

Toxicity

ExcerptReferenceRelevance
" No severe adverse events were observed."( Efficacy and safety of treating chronic nonspecific low back pain with radial extracorporeal shock wave therapy (rESWT), rESWT combined with celecoxib and eperisone (C + E) or C + E alone: a prospective, randomized trial.
Feng, Z; Guo, X; Li, L; Li, Y; Peng, Z; Schmitz, C; Yan, Z; Yang, Y; Zhang, Y, 2021
)
0.82

Pharmacokinetics

No clinically significant changes were noted in the pharmacokinetic interactions of pelubiprofen and eperisone hydrochloride between monotherapy and combination therapy. The geometric mean ratios (90% CIs) of the Cmax and AUC0-∞ values for eper isone were 1.

ExcerptReferenceRelevance
" The main pharmacokinetics parameters T1/2, Tmax and Cmax were (2."( [Pharmacokinetics and bioequivalence of eperisone hydrochloride tablet in healthy subjects].
Ding, L; Gao, JM; Li, J; Shen, JP; Wei, X; Zhang, SQ; Zhang, YD, 2004
)
0.59
" Although eperisone hydrochloride and aceclofenac are frequently coadministered, no published studies have reported on the pharmacokinetic interactions between these 2 drugs."( Pharmacokinetic interactions between eperisone hydrochloride and aceclofenac: a randomized, open-label, crossover study of healthy Korean men.
Bae, KS; Choi, HY; Kim, MJ; Kim, SE; Kim, YH; Lim, HS; Noh, YH; Park, KM, 2013
)
1.07
"The aim of this study was to investigate any pharmacokinetic interactions between eperisone hydrochloride and aceclofenac in healthy Korean men."( Pharmacokinetic interactions between eperisone hydrochloride and aceclofenac: a randomized, open-label, crossover study of healthy Korean men.
Bae, KS; Choi, HY; Kim, MJ; Kim, SE; Kim, YH; Lim, HS; Noh, YH; Park, KM, 2013
)
0.89
" Pharmacokinetic analyses were conducted using noncompartmental methods."( Pharmacokinetic interactions between eperisone hydrochloride and aceclofenac: a randomized, open-label, crossover study of healthy Korean men.
Bae, KS; Choi, HY; Kim, MJ; Kim, SE; Kim, YH; Lim, HS; Noh, YH; Park, KM, 2013
)
0.66
"No clinically significant pharmacokinetic differences exist between 150 mg eperisone hydrochloride and 200 mg aceclofenac when administrated as a monotherapy or in combination."( Pharmacokinetic interactions between eperisone hydrochloride and aceclofenac: a randomized, open-label, crossover study of healthy Korean men.
Bae, KS; Choi, HY; Kim, MJ; Kim, SE; Kim, YH; Lim, HS; Noh, YH; Park, KM, 2013
)
0.89
" No published data are yet available, however, regarding the pharmacokinetic interactions between these 2 drugs when administered concurrently."( Pharmacokinetic Interactions Between Pelubiprofen and Eperisone Hydrochloride: A Randomized, Open-label, Crossover Study of Healthy Korean Men.
Chung, EK; Kim, HS; Kim, JI; Lee, KT; Noh, GJ; Ryu, JH, 2017
)
0.7
" Pharmacokinetic analyses were conducted by using noncompartmental methods."( Pharmacokinetic Interactions Between Pelubiprofen and Eperisone Hydrochloride: A Randomized, Open-label, Crossover Study of Healthy Korean Men.
Chung, EK; Kim, HS; Kim, JI; Lee, KT; Noh, GJ; Ryu, JH, 2017
)
0.7
"No clinically significant changes were noted in the pharmacokinetic interactions of pelubiprofen, the major active metabolite of pelubiprofen (trans-alcohol pelubiprofen), and eperisone hydrochloride between monotherapy and combination therapy with 45-mg sustained-release pelubiprofen and 75-mg sustained-release eperisone hydrochloride."( Pharmacokinetic Interactions Between Pelubiprofen and Eperisone Hydrochloride: A Randomized, Open-label, Crossover Study of Healthy Korean Men.
Chung, EK; Kim, HS; Kim, JI; Lee, KT; Noh, GJ; Ryu, JH, 2017
)
0.9

Bioavailability

Oral eperisone has a very low bioavailability and short muscle relaxant activity, because of the profound intestinal first-pass metabolism. Clinical myotonolytic activity would only be expected at high doses.

ExcerptReferenceRelevance
" Similarly, clinical myotonolytic activity of eperisone would only be expected at high doses unless its functional bioavailability were to be much better in man than in either the mouse or rabbit."( Comparison of the myotonolytic activity of tizanidine, eperisone and afloqualone in mouse and rabbit.
Coward, DM; White, TG,
)
0.64
" However, oral eperisone has a very low bioavailability and short muscle relaxant activity, because of the profound intestinal first-pass metabolism."( Transdermal eperisone elicits more potent and longer-lasting muscle relaxation than oral eperisone.
Han, OY; Jang, CG; Kim, JJ; Lee, SH; Lee, SJ; Lee, SY; Lee, WS; Lim, SC; Park, HY; Shin, YH; Yang, SI, 2004
)
1.06
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" No significant change of the SLR was observed when dosage was less than 150 mg."( [Effects of muscle relaxant E-0646 on human stretch reflex and responses].
Iwase, S; Mano, T; Yamazaki, Y, 1991
)
0.28
" To improve the efficacy and compliance of eperisone, we designed a new dosage form, a transdermal patch, and evaluated the efficacy of the eperisone patch with the muscle relaxant activity of rats."( Transdermal eperisone elicits more potent and longer-lasting muscle relaxation than oral eperisone.
Han, OY; Jang, CG; Kim, JJ; Lee, SH; Lee, SJ; Lee, SY; Lee, WS; Lim, SC; Park, HY; Shin, YH; Yang, SI, 2004
)
0.97
"Understanding drug degradation in the pharmaceutical dosage forms is critical as it has significant impacts on drug efficacy, safety profile and storage conditions."( The use of HPLC/MS, GC/MS, NMR, UV and IR to identify a degradation product of eperisone hydrochloride in the tablets.
Chen, Y; Ding, L; Wang, X; Yang, Z, 2008
)
0.57
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
piperidines
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic ring.
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
gemininHomo sapiens (human)Potency37.58570.004611.374133.4983AID624297
acetylcholinesteraseHomo sapiens (human)Potency19.00180.002541.796015,848.9004AID1347395; AID1347397; AID1347398
TDP1 proteinHomo sapiens (human)Potency29.85540.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency33.49150.000221.22318,912.5098AID1259243
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency29.84930.001022.650876.6163AID1224838; AID1224893
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency28.18380.01237.983543.2770AID1346984
retinoid X nuclear receptor alphaHomo sapiens (human)Potency21.31380.000817.505159.3239AID1159527
pregnane X nuclear receptorHomo sapiens (human)Potency29.84930.005428.02631,258.9301AID1346982
cytochrome P450 2D6Homo sapiens (human)Potency0.87090.00108.379861.1304AID1645840
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency0.00060.023723.228263.5986AID743223
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency33.49150.001723.839378.1014AID743083
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency30.04740.000323.4451159.6830AID743065; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency24.41070.000627.21521,122.0200AID743202; AID743219
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency10.00000.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC50 (µMol)2.33800.00001.23267.7930AID625152
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.83100.00000.690210.0000AID625152
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)4.90340.00002.015110.0000AID625249
Alpha-2B adrenergic receptorHomo sapiens (human)IC50 (µMol)3.03400.00001.23808.1590AID625202
Alpha-2B adrenergic receptorHomo sapiens (human)Ki1.38500.00020.725710.0000AID625202
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC50 (µMol)0.00410.00030.70285.3660AID625223
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.00170.00000.490110.0000AID625223
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (49)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of heart contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
response to virusMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M2Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
arrestin family protein bindingMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (30)

Processvia Protein(s)Taxonomy
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
clathrin-coated endocytic vesicle membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
asymmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
symmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
neuronal cell bodyMuscarinic acetylcholine receptor M2Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M2Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M2Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (34)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (90)

TimeframeStudies, This Drug (%)All Drugs %
pre-199014 (15.56)18.7374
1990's19 (21.11)18.2507
2000's17 (18.89)29.6817
2010's25 (27.78)24.3611
2020's15 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 93.76

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index93.76 (24.57)
Research Supply Index4.71 (2.92)
Research Growth Index4.72 (4.65)
Search Engine Demand Index166.35 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (93.76)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials19 (20.88%)5.53%
Trials0 (0.00%)5.53%
Reviews2 (2.20%)6.00%
Reviews0 (0.00%)6.00%
Case Studies13 (14.29%)4.05%
Case Studies0 (0.00%)4.05%
Observational1 (1.10%)0.25%
Observational0 (0.00%)0.25%
Other56 (61.54%)84.16%
Other9 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (7)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Evaluation of Efficacy and Tolerability of a Fixed Dose Combination of Eperisone Hydrochloride and Diclofenac Sodium in the Treatment of Acute Musculoskeletal Spasm Associated With Low Back Pain: An Observer Blind, Prospective, Randomized, Controlled Stud [NCT01300312]Phase 3239 participants (Actual)Interventional2011-02-28Completed
A Clinical Study in Healthy Male Volunteers to Compare the Bioequivalence of Fixed Dose Combination of Eperisone Hydrochloride 50mg Plus Diclofenac Sodium 50mg as Capsule With Eperisone Hydrochloride 50mg and Diclofenac Sodium 50mg Tablets Under Fasting C [NCT01306318]24 participants (Actual)Interventional2011-02-28Completed
A Single-Center, Randomized, Double-Blind, Parallel, Pilot Study to Evaluate the Efficacy and Safety of Fixed Dose Combination of DW340 in Patients With Acute Low Back Pain [NCT03424707]Phase 245 participants (Actual)Interventional2016-03-04Completed
Partial Replicated Crossover Clinical Study to Compare Pharmacokinetic Characteristics of Eperisone and Aceclofenac With NVP-1203 Treatment to Those of Co-administration of Eperisone Hydrochloride Slow Release and Aceclofenac in Volunteers [NCT02289274]Phase 10 participants (Actual)Interventional2019-11-30Withdrawn(stopped due to internal decision)
A Multicenter, Randomized, Double-blinded, Parallel, Active-controlled, Phase Lll Clinical Trial to Evaluate the Efficacy and Safety of DW-1030 and Eperisone HCl in Acute Back Pain Patients [NCT02040415]Phase 3242 participants (Actual)Interventional2014-03-31Completed
Evaluation of Eperisone HCl in the Treatment of Acute Musculoskeletal Spasm Associated With Low Back Pain [NCT00327730]Phase 3240 participants (Actual)Interventional2006-04-30Completed
A Prospective, Randomized, Controlled, Single Centre Trial to Assess the Efficacy and Safety of Radial Extracorporeal Shock Wave Therapy in Patients With Chronic Non-specific Low Back Pain [NCT03337607]150 participants (Anticipated)Interventional2017-11-13Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]