Page last updated: 2024-08-03 03:31:01

gr 82334

Description

GR 82334: tachykinin NK-1 receptor antagonist [MeSH]

Cross-References

ID SourceID
PubMed CID16130972
SCHEMBL ID7945525
MeSH IDM0211648

Synonyms (11)

Synonym
physalaemin(1-11), d-pro(9)(spiro-gamma-lactam)leu(10)-trp(11)-
physalemin, 9-deglycine-10-((5s)-6-oxo-l-alpha-(2-methylpropyl)-1,7-diazaspiro(4.4)nonane-7-acetic acid)-11-l-tryptophanamide-
gr 82334
129623-01-4
SCHEMBL7945525
AKOS024456738
DTXSID10156209
gr 82334, >=95%
gr82334
xadpnkfyxl w
l-tryptophanamide,5-oxo-l-prolyl-l-alanyl-l-a-aspartyl-l-prolyl-l-asparaginyl-l-lysyl-l-phenylalanyl-l-tyrosyl-(as,5s)-a-(2-methylpropyl)-6-oxo-1,7-diazaspiro[4.4]nonane-7-acetyl-

Research

Studies (65)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's43 (66.15)18.2507
2000's17 (26.15)29.6817
2010's5 (7.69)24.3611
2020's0 (0.00)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other65 (100.00%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
gamma-aminobutyric acidamino acid zwitterion;
gamma-amino acid;
monocarboxylic acid
human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
1995199529.0low001000
pyridoxal phosphatemethylpyridines;
monohydroxypyridine;
pyridinecarbaldehyde;
vitamin B6 phosphate
coenzyme;
cofactor;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
1999200024.5low002000
2-amino-5-phosphonovaleratenon-proteinogenic alpha-amino acidNMDA receptor antagonist1993199430.5low002000
sk&f-38393benzazepine;
catechols;
secondary amino compound
1997199727.0low001000
4-aminopyridineaminopyridine;
aromatic amine
avicide;
orphan drug;
potassium channel blocker
1993199729.0low002000
7-nitroindazole2004200420.0low000100
bisindolylmaleimide i2003200321.0low000100
celecoxiborganofluorine compound;
pyrazoles;
sulfonamide;
toluenes
cyclooxygenase 2 inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
2004200420.0low000100
thiorphanN-acyl-amino acid1997199727.0low001000
fenvaleratearomatic ether;
carboxylic ester;
monochlorobenzenes
pyrethroid ester acaricide;
pyrethroid ester insecticide
2001200123.0low000100
guanethidineazocanes;
guanidines
adrenergic antagonist;
antihypertensive agent;
sympatholytic agent
1995199529.0low001000
1-(5-isoquinolinesulfonyl)-2-methylpiperazineisoquinolines;
N-sulfonylpiperazine
EC 2.7.11.13 (protein kinase C) inhibitor2009200915.0low000100
haloperidolaromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol
antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
1997199727.0low001000
hexamethoniumquaternary ammonium salt1993199331.0low001000
lidocainebenzenes;
monocarboxylic acid amide;
tertiary amino compound
anti-arrhythmia drug;
drug allergen;
environmental contaminant;
local anaesthetic;
xenobiotic
1996199628.0low001000
indomethacinaromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole
analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite;
xenobiotic
1995201121.0low001010
isoproterenolcatechols;
secondary alcohol;
secondary amino compound
beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
sympathomimetic agent
1994199430.0low001000
ketanserinaromatic ketone;
organofluorine compound;
piperidines;
quinazolines
alpha-adrenergic antagonist;
antihypertensive agent;
cardiovascular drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
1997199727.0low001000
mexiletinearomatic ether;
primary amino compound
anti-arrhythmia drug2001200123.0low000100
nicardipinebenzenes;
C-nitro compound;
diester;
dihydropyridine;
methyl ester;
tertiary amino compound
2003200321.0low000100
nifedipineC-nitro compound;
dihydropyridine;
methyl ester
calcium channel blocker;
human metabolite;
tocolytic agent;
vasodilator agent
1994199529.5low002000
potassium chlorideinorganic chloride;
inorganic potassium salt;
potassium salt
fertilizer1999199925.0low001000
pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acidarenesulfonic acid;
azobenzenes;
methylpyridines;
monohydroxypyridine;
organic phosphate;
pyridinecarbaldehyde
purinergic receptor P2X antagonist1999200024.5low002000
proglumidebenzamides;
dicarboxylic acid monoamide;
glutamine derivative;
racemate
anti-ulcer drug;
cholecystokinin antagonist;
cholinergic antagonist;
delta-opioid receptor agonist;
drug metabolite;
gastrointestinal drug;
opioid analgesic;
xenobiotic metabolite
1993199331.0low001000
ritanserinorganofluorine compound;
piperidines;
thiazolopyrimidine
antidepressant;
antipsychotic agent;
anxiolytic drug;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
1997199727.0low001000
suraminnaphthalenesulfonic acid;
phenylureas;
secondary carboxamide
angiogenesis inhibitor;
antinematodal drug;
antineoplastic agent;
apoptosis inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
GABA antagonist;
GABA-gated chloride channel antagonist;
purinergic receptor P2 antagonist;
ryanodine receptor agonist;
trypanocidal drug
1995201516.0low001020
urethanecarbamate esterfungal metabolite;
mutagen
1996199628.0low001000
corticosterone11beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone
human metabolite;
mouse metabolite
2007200717.0low000100
carbacholammonium salt;
carbamate ester
cardiotonic drug;
miotic;
muscarinic agonist;
nicotinic acetylcholine receptor agonist;
non-narcotic analgesic
1993199331.0low001000
lysineaspartate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
lysine;
organic molecular entity;
proteinogenic amino acid
algal metabolite;
anticonvulsant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
2004200420.0low000100
adenosine diphosphateadenosine 5'-phosphate;
purine ribonucleoside 5'-diphosphate
fundamental metabolite;
human metabolite
1995199529.0low001000
phenylephrinephenols;
phenylethanolamines;
secondary amino compound
alpha-adrenergic agonist;
cardiotonic drug;
mydriatic agent;
nasal decongestant;
protective agent;
sympathomimetic agent;
vasoconstrictor agent
2001200123.0low000100
argininearginine;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid
biomarker;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical
1995199529.0low001000
quinoxalinesmancude organic heterobicyclic parent;
naphthyridine;
ortho-fused heteroarene
2009200915.0low000100
pyrrolidonecarboxylic acid5-oxoproline;
L-proline derivative;
non-proteinogenic L-alpha-amino acid
algal metabolite1993199729.5low004000
quinuclidinesquinuclidines;
saturated organic heterobicyclic parent
1997200624.0low002100
indazolesindazole2004200420.0low000100
toluene 2,4-diisocyanatetoluene meta-diisocyanateallergen;
hapten
1994199430.0low001000
copper sulfatemetal sulfateemetic;
fertilizer;
sensitiser
1999199925.0low001000
substance ppeptideneurokinin-1 receptor agonist;
neurotransmitter;
vasodilator agent
1993201426.0medium0027910
mezlocillin2004200420.0low000100
mifepristone3-oxo-Delta(4) steroid;
acetylenic compound;
tertiary amino compound
abortifacient;
contraceptive drug;
hormone antagonist;
synthetic oral contraceptive
2007200717.0low000100
loxiglumideorganic molecular entity1993199331.0low001000
mesulergineergot alkaloid;
sulfamides
antiparkinson drug;
dopamine agonist;
serotonergic antagonist
1997199727.0low001000
nicotine3-(1-methylpyrrolidin-2-yl)pyridineanxiolytic drug;
biomarker;
immunomodulator;
mitogen;
neurotoxin;
nicotinic acetylcholine receptor agonist;
peripheral nervous system drug;
phytogenic insecticide;
plant metabolite;
psychotropic drug;
teratogenic agent;
xenobiotic
1999199925.0low001000
alpha,beta-methyleneadenosine 5'-triphosphatenucleoside triphosphate analogue2010201014.0low000100
cp 963451994200228.1low006100
1-(2-(3-(4-methoxyphenyl)propoxy)-4-methoxyphenylethyl)-1h-imidazoleether;
imidazoles;
monomethoxybenzene
TRP channel blocker2003200321.0low000100
sr 489681994199629.3low003000
fluorocitratecarbonyl compound2004200420.0low000100
7,7-diphenyl-2-(1-imino-2-(2-methoxyphenyl)ethyl)perhydroisoindol-4-one1993200526.2low006200
fk 888peptide1994199927.7low003000
senktide1993200028.0low006000
sr 1403331997199727.0low002000
gr 736321993200028.8low006000
substance p, methyl ester-1993199331.0low001000
neurokinin a (4-10), beta-ala(8)-1995199529.0low001000
neurokinin a(4-10), tyr(5)-trp(6,8,9)-lys(10)-1993200426.6medium005300
l 7036062006200618.0low000100
omega-n-methylarginineamino acid zwitterion;
arginine derivative;
guanidines;
L-arginine derivative;
non-proteinogenic L-alpha-amino acid
1997199727.0low001000
substance p, pro(9)-1994199430.0low001000
substance p, sar(9)-met(o2)(11)-1993201025.9low007300
atropine1993199928.5low008000
bradykininoligopeptidehuman blood serum metabolite;
vasodilator agent
1993199630.0low003000
inositol 1,4,5-trisphosphatemyo-inositol trisphosphatemouse metabolite1996199628.0low001000
nitroarginineguanidines;
L-arginine derivative;
N-nitro compound;
non-proteinogenic L-alpha-amino acid
1995200026.7low003000
ryanodine2003200321.0low000100
devazepide1,4-benzodiazepinone;
indolecarboxamide
antineoplastic agent;
apoptosis inducer;
cholecystokinin antagonist;
gastrointestinal drug
1999199925.0low001000
cocainebenzoate ester;
methyl ester;
tertiary amino compound;
tropane alkaloid
adrenergic uptake inhibitor;
central nervous system stimulant;
dopamine uptake inhibitor;
environmental contaminant;
local anaesthetic;
mouse metabolite;
plant metabolite;
serotonin uptake inhibitor;
sodium channel blocker;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic
2005200618.5low000200
tetragastrinpeptidyl amide;
tetrapeptide
anxiogenic;
human metabolite
1994199430.0low001000
capsaicincapsaicinoidnon-narcotic analgesic;
TRPV1 agonist;
voltage-gated sodium channel blocker
1992200029.3low0010000
neurokinin a (3-10), lysyl(3)-glycyl(8)-r-lactam-leucine(9)-1993200327.7medium002100
substance p (4-11), beta-ala(4)-sar(9)-met(02)(11)-2006200618.0high000100
2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxalinenaphthalenes;
sulfonic acid derivative
2009200915.0low000100
ovalbumin2007200717.0low000100
adp beta s1995199529.0low001000
cp 999941995199927.0low002000
neurokinin a1993200428.1low0011300
kn 62piperazines2009200915.0low000100
gr 948001994199529.5medium002000
tetrodotoxinazatetracycloalkane;
oxatetracycloalkane;
quinazoline alkaloid
animal metabolite;
bacterial metabolite;
marine metabolite;
neurotoxin;
voltage-gated sodium channel blocker
1993200128.0low004100
dizocilpine maleatemaleate salt;
tetracyclic antidepressant
anaesthetic;
anticonvulsant;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist
2001200421.5low000200
cyclo(gln-trp-phe-gly-leu-met)1993199530.0low002000
ergolinediamine;
ergoline alkaloid;
indole alkaloid fundamental parent;
indole alkaloid;
organic heterotetracyclic compound
1997199727.0low001000
win 517081997201120.0low001010
sr 1428011997200025.3low003000
(2s,3s)-2-phenyl-3-((5-trifluoromethoxy-2-methoxy)benzylamino)piperidine1999199925.0low001000
sincalideoligopeptide2000200024.0low001000
men 114201997200125.0low002100
eledoisinpeptide2004200420.0low000100
bufokinin2004200420.0medium000100
physalaemin1992201525.2high00451640
cholecystokinin1999199925.0low001000
iberiotoxin2003200321.0low000100
septide1993199729.5low004000
gr 712511995199529.0low001000
piperidines1994200027.2low0010000
vasoactive intestinal peptide2000200621.0low001100
pyrethrins2001200123.0low000100
tan 671999199925.0low001000
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Abnormal Deep Tendon Reflex02001200123.0low000100
Ache02001201417.8low000310
Adjuvant Arthritis02011201113.0low000010
Air Sickness01999199925.0low001000
Allodynia01999201119.8low001310
Anesthesia01996199628.0low001000
Apnea, Obstructive Sleep02014201410.0low000010
Asthma02007200717.0low000100
Asthma, Bronchial02007200717.0low000100
Bladder Disorder, Neurogenic02001200123.0low000100
Blood Pressure, High02000200024.0low001000
Bronchial Spasm01994199430.0low001000
Bronchospasm01994199430.0low001000
Cocaine Abuse02005200519.0low000100
Cocaine-Related Disorders02005200519.0low000100
Cystitis01994201420.0low001010
Disease Models, Animal0201420159.5low000020
Emesis01999199925.0low001000
Erectile Dysfunction0201520159.0low000010
Extravasation of Contrast Media01994199430.0low001000
Hypertension02000200024.0low001000
Impotence0201520159.0low000010
Inflammation02011201113.0low000010
Injuries, Spinal Cord02001201516.0low000110
Innate Inflammatory Response02011201113.0low000010
Motion Sickness01999199925.0low001000
Muscle Contraction01992200427.3high0015400
Muscle Relaxation01994199430.0low001000
Pain02001201417.8low000310
Recrudescence02005200519.0low000100
Reflex, Abnormal02001200123.0low000100
Sensitivity and Specificity01995199628.5low002000
Sleep Apnea, Obstructive02014201410.0low000010
Spinal Cord Injuries02001201516.0low000110
Urinary Bladder, Neurogenic02001200123.0low000100
Urinary Incontinence01994199430.0low001000
Vomiting01999199925.0low001000

Dosage (1)

ArticleYear
CGRP(8-37) and CGRP(32-37) contract the iris sphincter in the rabbit eye: antagonism by spantide and GR82334.
Regulatory peptides, , Nov-19, Volume: 49, Issue:1
1993