Compounds > rpr 100893
Page last updated: 2024-11-07

rpr 100893

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

RPR 100893: a non-peptide selective antagonist of human NK1 receptors; a 7,7,4-triarylperhydroisoindol-4-ol; RPR 103253 is an enantiomer of RPR 100893; Dapitant is tradename [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID132961
CHEMBL ID38824
SCHEMBL ID121135
MeSH IDM0237482

Synonyms (25)

Synonym
(3as,4s,7as)-hexahydro-2-((alphas)-o-methoxyhydratropoyl)-4-(o-methoxyphenyl)-7,7-diphenyl-4-isoindolinol
dapitant [inn]
rpr 103253
rpr-103253
1h-isoindol-4-ol, octahydro-4-(2-methoxyphenyl)-2-(2-(2-methoxyphenyl)-1-oxopropyl)-7,7-diphenyl-, (3as-(2(r*),3aalpha,4beta,7aalpha))-
nrd5xf638p ,
153438-49-4
unii-nrd5xf638p
rpr 100893
dapitant
CHEMBL38824 ,
rpr-100893
(2s)-1-[(3as,4s,7as)-4-hydroxy-4-(2-methoxyphenyl)-7,7-diphenyl-1,3,3a,5,6,7a-hexahydroisoindol-2-yl]-2-(2-methoxyphenyl)propan-1-one
1-[4-hydroxy-4-(2-methoxy-phenyl)-7,7-diphenyl-octahydro-isoindol-2-yl]-2-(2-methoxy-phenyl)-propan-1-one
(s)-1-[(3as,7as)-4-hydroxy-4-(2-methoxy-phenyl)-7,7-diphenyl-octahydro-isoindol-2-yl]-2-(2-methoxy-phenyl)-propan-1-one
bdbm50284876
SCHEMBL121135
(3as,4s,7as)-hexahydro-2-((.alpha.s)-o-methoxyhydratropoyl)-4-(o-methoxyphenyl)-7,7-diphenyl-4-isoindolinol
(3as,4s,7as)-7,7-diphenyl-4-(2-methoxyphenyl)-2-[(s)-2-(2-methoxyphenyl)propionyl]perhydroisoindol-4-ol
(3as,4s,7as)-7,7-diphenyl-4-(2-methoxyphenyl)-2-[(s)-2-(2methoxyphenyl)propionyl]perhydroisoindol-4-ol
CCIWVEMVBWEMCY-RCFOMQFPSA-N
(3as,4s,7as)-7,7-diphenyl-4-(2-methoxyphenyl)-2-[2-(2-methoxyphenyl)-(s)-propionyl]-perhydroisoindol-4-ol
rpr100893
Q1165545
(s)-1-((3as,4s,7as)-4-hydroxy-4-(2-methoxyphenyl)-7,7-diphenylhexahydro-1h-isoindol-2(3h)-yl)-2-(2-methoxyphenyl)propan-1-one

Research Excerpts

Treatment

ExcerptReferenceRelevance
"Pretreatment with RPR 100893 (1, 10 and 100 micrograms/kg, i.v.) but not its enantiomer (100 micrograms/kg, i.v.) 30 min prior to capsaicin injection significantly reduced the number of positive cells in the trigeminal nucleus caudalis (P < 0.01) in a dose-dependent manner, but not within area postrema or nucleus of the solitary tract."( The non-peptide neurokinin-1 antagonist, RPR 100893, decreases c-fos expression in trigeminal nucleus caudalis following noxious chemical meningeal stimulation.
Cutrer, FM; Garret, C; Moskowitz, MA; Moussaoui, S, 1995)		0.88
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's9 (69.23)18.2507
2000's4 (30.77)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.45

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.45 (24.57)
Research Supply Index2.71 (2.92)
Research Growth Index4.16 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.45)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (7.69%)5.53%
Reviews1 (7.69%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (84.62%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
valproic acid
Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem.		3.0910branched-chain fatty acid;
branched-chain saturated fatty acid		anticonvulsant;
antimanic drug;
EC 3.5.1.98 (histone deacetylase) inhibitor;
GABA agent;
neuroprotective agent;
psychotropic drug;
teratogenic agent
sumatriptan
Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.. sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults.		3.0910sulfonamide;
tryptamines		serotonergic agonist;
vasoconstrictor agent
pyrrolidonecarboxylic acid
Pyrrolidonecarboxylic Acid: A cyclized derivative of L-GLUTAMIC ACID. Elevated blood levels may be associated with problems of GLUTAMINE or GLUTATHIONE metabolism.. 5-oxo-L-proline : An optically active form of 5-oxoproline having L-configuration.		1.99105-oxoproline;
L-proline derivative;
non-proteinogenic L-alpha-amino acid		algal metabolite
quinuclidines
Quinuclidines: A class of organic compounds which contain two rings that share a pair of bridgehead carbon atoms and contains an amine group.		2.4120quinuclidines;
saturated organic heterobicyclic parent
substance p
[no description available]		9.7671peptideneurokinin-1 receptor agonist;
neurotransmitter;
vasodilator agent
sr 48968
SR 48968: structure given in first source; neurokinin A antagonist; tachykinin receptor antagonist; SR 48965 is the inactive R-enantiomer of SR 48968		2.420
7,7-diphenyl-2-(1-imino-2-(2-methoxyphenyl)ethyl)perhydroisoindol-4-one
7,7-diphenyl-2-(1-imino-2-(2-methoxyphenyl)ethyl)perhydroisoindol-4-one: structure given in first source; RP 68651 is the inactive (3aS,7aS)-isomer; substance P antagonist		2.6830
sr 140333
SR 140333: SR-140603 is the (R)-antipode of SR-140333; a neurokinin-1 receptor antagonist		2.4120
neurokinin a (4-10), beta-ala(8)-
neurokinin A (4-10), beta-Ala(8)-: selective NK-2 tachykinin receptor		1.9910
proline
Proline: A non-essential amino acid that is synthesized from GLUTAMIC ACID. It is an essential component of COLLAGEN and is important for proper functioning of joints and tendons.. proline : An alpha-amino acid that is pyrrolidine bearing a carboxy substituent at position 2.		2.420amino acid zwitterion;
glutamine family amino acid;
L-alpha-amino acid;
proline;
proteinogenic amino acid		algal metabolite;
compatible osmolytes;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
capsaicin
ALGRX-4975: an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief. capsaicinoid : A family of aromatic fatty amides produced as secondary metabolites by chilli peppers.		2.3920capsaicinoidnon-narcotic analgesic;
TRPV1 agonist;
voltage-gated sodium channel blocker
cp 99994
3-(2-methoxybenzylamino)-2-phenylpiperidine: selective NK(1) receptor antagonist; CP-100263 is the inactive enantiomer		1.9810
neurokinin a
Neurokinin A: A mammalian neuropeptide of 10 amino acids that belongs to the tachykinin family. It is similar in structure and action to SUBSTANCE P and NEUROKININ B with the ability to excite neurons, dilate blood vessels, and contract smooth muscles, such as those in the BRONCHI.		1.9910
sr 142801
SR 142801: SR 142806 is the (R)-enantiomer; structure given in first source; neurokinin-3 receptor antagonist		210
sdz nkt 343
SDZ NKT 343: structure in first source		2.420
septide
[no description available]		1.9910
piperidines
Piperidines: A family of hexahydropyridines.		3.0950
ConditionIndicatedRelationship StrengthStudiesTrials
Abdominal Migraine
[description not available]		0531
Migraine Disorders
A class of disabling primary headache disorders, characterized by recurrent unilateral pulsatile headaches. The two major subtypes are common migraine (without aura) and classic migraine (with aura or neurological symptoms). (International Classification of Headache Disorders, 2nd ed. Cephalalgia 2004: suppl 1)		0531
Ache
[description not available]		01.9810
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		01.9810
Blood Pressure, Low
[description not available]		01.9910
Hypotension
Abnormally low BLOOD PRESSURE that can result in inadequate blood flow to the brain and other vital organs. Common symptom is DIZZINESS but greater negative impacts on the body occur when there is prolonged depravation of oxygen and nutrients.		01.9910
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.420
Allodynia
[description not available]		02.420
Nerve Pain
[description not available]		01.9910
Neuralgia
Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.		01.9910
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		0210