Page last updated: 2024-12-07

msh release-inhibiting hormone

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

Msh release-inhibiting hormone (MSH-RIH) is a peptide hormone that plays a crucial role in regulating the release of melanocyte-stimulating hormone (MSH) from the pituitary gland. MSH-RIH is synthesized in the hypothalamus and acts as a paracrine factor, meaning it exerts its effects on nearby cells. It has been shown to inhibit the release of MSH by directly interacting with melanotrophs, the cells in the pituitary gland that produce and release MSH. The importance of MSH-RIH lies in its role in regulating pigmentation, energy metabolism, and other physiological processes influenced by MSH. The study of MSH-RIH is significant because it provides insights into the complex mechanisms that govern hormone secretion and its effects on various bodily functions. Furthermore, understanding MSH-RIH's role in pigmentation could lead to the development of novel therapeutic strategies for treating skin disorders.'

Cross-References

ID SourceID
PubMed CID92910
CHEMBL ID317488
CHEBI ID168693
SCHEMBL ID362530
MeSH IDM0014157

Synonyms (49)

Synonym
CHEMBL317488 ,
CHEBI:168693
pro-leu-gly amide
mif-1
2002-44-0
l-prolyl-l-leucylglycinamide
(s)-pyrrolidine-2-carboxylic acid [(s)-1-(carbamoylmethyl-carbamoyl)-3-methyl-butyl]-amide
bdbm50060601
l-pro-l-leu-gly-nh2
pyrrolidine-2-carboxylic acid [1-(carbamoylmethyl-carbamoyl)-3-methyl-butyl]-amide
6-((e)-3-oxo-3-phenyl-propenyl)-1h-pyrimidine-2,4-dione
(e)-6-(3-oxo-3-phenylprop-1-enyl)pyrimidine-2,4(1h,3h)-dione
mif-i
AKOS015955826
msh-release inhibiting factor i
unii-3ky24b4q62
oxytocin c-terminal tripeptide
2-pyrrolidinecarboxamide, n-(1-((carbamoylmethyl)carbamoyl)-3-methylbutyl)-
3ky24b4q62 ,
7-9-oxytocin
glycinamide, l-prolyl-l-leucyl-
melanostatin i (ox)
prolylleucylglycine amide
prolyl-l-leucyl-glycinamide, l-
einecs 217-902-7
l-prolyl-l-leucylglycylamide
l-proline-l-leucine-glycine-amide
STL372235
BBL033793
melanostatin mif-i
mif-i, (-)-
melanostatin mif-i [mi]
msh release-inhibiting factor i
SCHEMBL362530
(s)-n-((s)-1-((2-amino-2-oxoethyl)amino)-4-methyl-1-oxopentan-2-yl)pyrrolidine-2-carboxamide ,
c13h24n4o3
DTXSID20173841
mfcd00037866
(2s)-n-(carbamoylmethyl)-4-methyl-2-[(2s)-pyrrolidin-2-ylformamido]pentanamide
(s)-n-((s)-1-(2-amino-2-oxoethylamino)-4-methyl-1-oxopentan-2-yl)pyrrolidine-2-carboxamide
HY-107663
NS-04720
(2s)-n-(carbamoylmethyl)-4-methyl-2-{[(2s)-pyrrolidin-2-yl]formamido}pentanamide
HB1874
A14870
mfcd08282654
CS-0029128
PD070730
EN300-302728

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Analogues 3-6 and 8 exhibited dose-response curves that were bell-shaped in nature with the maximum effect occurring at a concentration of 1 microM."( Synthesis and dopamine receptor modulating activity of lactam conformationally constrained analogues of Pro-Leu-Gly-NH2.
Johnson, RL; Mishra, RK; Sreenivasan, U, 1993
)
0.29
" Like PLG the dose-response curves for 3 and 4 were bell-shaped in nature with the maximum effect occurring at a concentration of 1 microM."( Bicyclic thiazolidine lactam peptidomimetics of the dopamine receptor modulating peptide Pro-Leu-Gly-NH2.
Bontems, RJ; Johnson, RL; McIntee, E; Mishra, RK; Subasinghe, NL, 1993
)
0.29
" Peptidomimetics 3 and 4 were evaluated in vivo as modulators of apomorphine-induced rotational behavior in the 6-hydroxydopamine-lesioned rat model of hemiparkinsonism, and each affected the rotational behavior in a bell-shaped dose-response relationship producing increases of 95 +/- 31% (0."( Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
Gleason, WB; Johnson, RL; Khalil, EM; Mishra, RK; Nair, VD; Ojala, WH; Pradhan, A, 1999
)
0.3
" The dose-response curve of the mimetic was found to exhibit a down-turn phase, similar to that of PLG."( Design, synthesis and evaluation of a PLG tripeptidomimetic based on a pyridine scaffold.
Boström, D; Del Tredici, AL; Kihlberg, J; Luthman, K; Mohell, N; Saitton, S; Vollinga, RC, 2004
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
oligopeptideA peptide containing a relatively small number of amino acids.
[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 (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.06010.00000.887110.0000AID61465
D(2) dopamine receptorHomo sapiens (human)Ki0.03400.00000.651810.0000AID61461; AID61462; AID61463; AID61464; AID61465; AID61466; AID63986
D(2) dopamine receptorBos taurus (cattle)Ki0.03400.00000.58366.1000AID62345; AID62470; AID62471; AID62474; AID62476; AID62477; AID62482
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)Ki0.06000.00161.02535.0119AID62345; AID62477
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
D(2) dopamine receptorHomo sapiens (human)EC50 (µMol)0.17000.00000.18743.9000AID1807005
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (101)

Processvia Protein(s)Taxonomy
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(2) dopamine receptorBos taurus (cattle)
negative regulation of prolactin secretionD(2) dopamine receptorBos taurus (cattle)
negative regulation of lactationD(2) dopamine receptorBos taurus (cattle)
positive regulation of mammary gland involutionD(2) dopamine receptorBos taurus (cattle)
hyaloid vascular plexus regressionD(2) dopamine receptorBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (21)

Processvia Protein(s)Taxonomy
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
Golgi membraneD(2) dopamine receptorBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (81)

Assay IDTitleYearJournalArticle
AID1136071Potentiation of dl-DOPA-induced behavioral effects in ICR mouse assessed as marked piloerection, profuse salivation, marked increased irritability and reactivity, jumping, squeaking and aggressive fighting at 0.1 mg/kg, ip administered 1 hr prior to dl-DO1978Journal of medicinal chemistry, Feb, Volume: 21, Issue:2
Study of the structural requirements for dopa potentiation and oxotremorine antagonism by L-prolyl-L-leucylglycinamide.
AID62460In vitro ability to enhance the binding of [3H]ADTN to dopamine receptor obtained from bovine caudate membranes at a concentration of 10E-6 M1993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Synthesis and dopamine receptor modulating activity of lactam conformationally constrained analogues of Pro-Leu-Gly-NH2.
AID61473Percent of Dopamine receptor D2 in low affinity state for the compound in presence of Gpp(NH)p1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID61467Percent of Dopamine receptor D2 in high affinity state for the compound in absence of Gpp(NH)p1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID226423Ratio of the high affinity state over low affinity state of dopamine D2 receptor in the absence of Gpp(NH)p. (pretreatment with 100 nM of compound).1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID62470Inhibitory constant of compound in absence of Gpp(NH)p calculated for the high affinity components of the [3H]spiroperidol binding to Dopamine receptor D21997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID735546Analgesic activity in Wistar rats assessed as increase in mechanical nociceptive threshold at 1 mg/kg, ip measured after 15 mins by paw pressure test2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis of an MIF-1 analogue containing enantiopure (S)-α-trifluoromethyl-proline and biological evaluation on nociception.
AID774975Positive allosteric modulation of human dopamine D2S receptor expressed in CHO cell membranes assessed as stimulation of [3H]-NPA binding at 10'-8 to 10'-4 M after 60 mins by beta scintillation counting analysis2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis and allosteric modulation of the dopamine receptor by peptide analogs of L-prolyl-L-leucyl-glycinamide (PLG) modified in the L-proline or L-proline and L-leucine scaffolds.
AID587330Agonist activity at human dopamine D2 receptor at 10 nM2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Tripeptide motifs in biology: targets for peptidomimetic design.
AID226425Ratio of the high affinity state over low affinity state of dopamine D2 receptor in the presence of Gpp(NH)p. (pretreatment with 100 nM of compound).1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID231434RH/RL ratio of the compound1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID735539Analgesic activity in Wistar rats assessed as increase in mechanical nociceptive threshold at 1 mg/kg, ip treated 20 mins after 1 mg/kg, ip NO donor, L-arginine challenge measured after 15 to 45 mins by paw pressure test2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis of an MIF-1 analogue containing enantiopure (S)-α-trifluoromethyl-proline and biological evaluation on nociception.
AID61463Inhibitor constant of compound for high affinity component of [3H]spiroperidol/N-propylnorapomorphine binding to Dopamine receptor D2 in presence of Gpp(NH)p (pretreatment with 100 nM of compound)1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID62620Ability to enhance the binding of [3H]-ADTN to Dopamine receptor D2 isolated from bovine caudate membranes at 1 uM concentration1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and biological evaluation of analogues of Pro-Leu-Gly-NH2 modified at the leucyl residue.
AID62617Percentage of receptor in the low affinity form for the compound to Dopamine receptor D2 in presence of Gpp(NH)p1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID62301Compound was tested for enhancement of the binding of [3H]ADTN to dopamine receptors at concentration of 100 nM1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of Pro-Leu-Gly-NH2 analogues modified at the prolyl residue and evaluation of their effects on the receptor binding activity of the central dopamine receptor agonist, ADTN.
AID282084Activity at human dopamine D2 receptor in NIH/3T3 cells assessed as enhancement of NPA-stimulated beta-galactosidase activity at 50 nM after 5 days by R-SAT assay2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Design, synthesis and evaluation of a PLG tripeptidomimetic based on a pyridine scaffold.
AID61472Percent of Dopamine receptor D2 in low affinity state for the compound in absence of Gpp(NH)p (pretreatment with 100 nM of compound).1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID257907Stimulation of [3H]NPA binding to dopamine D2 receptor from bovine striatal membranes in presence of photoaffinity-labeling agents2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Design and synthesis of photoaffinity-labeling ligands of the L-prolyl-L-leucylglycinamide binding site involved in the allosteric modulation of the dopamine receptor.
AID62500Percentage of receptor in the high affinity form for the compound to Dopamine receptor D2 in presence of Gpp(NH)p (pre treated with 1 uM)1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID62305Compound was tested for enhancement of the binding of [3H]ADTN to dopamine receptors at concentration of 1 nM1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of Pro-Leu-Gly-NH2 analogues modified at the prolyl residue and evaluation of their effects on the receptor binding activity of the central dopamine receptor agonist, ADTN.
AID1136962Inhibition of oxotremorine-induced tremor in ip dosed NMRI mouse administered 1 hr prior to oxotremorine challenge1979Journal of medicinal chemistry, Aug, Volume: 22, Issue:8
Tripeptide analogues of melanocyte-stimulating hormone release-inhibiting hormone (Pro-Leu-Gly-NH2) as inhibitors of oxotremorine-induced tremor.
AID735538Analgesic activity in Wistar rats assessed as increase in latency of response to pain at 1 mg/kg, ip treated 20 mins after 10 mg/kg, ip NOS inhibitor, L-NAME challenge measured after 15 to 45 mins by hot plate test2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis of an MIF-1 analogue containing enantiopure (S)-α-trifluoromethyl-proline and biological evaluation on nociception.
AID62304Enhancement of [3H]-ADTN to dopamine receptors at concentration of 1 nM1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Dopamine receptor modulation by Pro-Leu-Gly-NH2 analogues possessing cyclic amino acid residues at the C-terminal position.
AID735545Analgesic activity in Wistar rats assessed as increase in latency of response to pain at 1 mg/kg, ip measured after 15 mins by hot plate test2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis of an MIF-1 analogue containing enantiopure (S)-α-trifluoromethyl-proline and biological evaluation on nociception.
AID280941Cytotoxicity against mouse L1210/0 cells after 48 hrs2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Probing the anticancer activity of nucleoside analogues: a QSAR model approach using an internally consistent training set.
AID62294Tested for ability to enhance the binding of the dopamine receptor agonist [3H]ADTN to striatal dopamine receptors in vitro1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Dopamine receptor modulation by a highly rigid spiro bicyclic peptidomimetic of Pro-Leu-Gly-NH2.
AID735537Analgesic activity in Wistar rats assessed as increase in latency of response to pain at 1 mg/kg, ip treated 20 mins after 1 mg/kg, ip NO donor, L-arginine challenge measured after 15 to 45 mins by hot plate test2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis of an MIF-1 analogue containing enantiopure (S)-α-trifluoromethyl-proline and biological evaluation on nociception.
AID282085Activity at human dopamine D2 receptor in NIH/3T3 cells assessed as enhancement of NPA-stimulated beta-galactosidase activity at 100 nM after 5 days by R-SAT assay2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Design, synthesis and evaluation of a PLG tripeptidomimetic based on a pyridine scaffold.
AID61471Percent of Dopamine receptor D2 in low affinity state for the compound in absence of Gpp(NH)p1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID257906Stimulation of [3H]NPA binding to dopamine D2 receptor in bovine striatal membranes2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Design and synthesis of photoaffinity-labeling ligands of the L-prolyl-L-leucylglycinamide binding site involved in the allosteric modulation of the dopamine receptor.
AID62299Ability to enhance the binding of [3H]- ADTN to dopamine receptor from freshly dissected bovine caudate at 1 uM; Range is 25-401993Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16
Bicyclic thiazolidine lactam peptidomimetics of the dopamine receptor modulating peptide Pro-Leu-Gly-NH2.
AID62477Inhibitory constant of compound in presence of Gpp(NH)p calculated for the low affinity components of the [3H]spiroperidol binding to Dopamine receptor D21997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID62303Compound was tested for enhancement of the binding of [3H]-ADTN to dopamine receptors at concentration of 10 nM1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of Pro-Leu-Gly-NH2 analogues modified at the prolyl residue and evaluation of their effects on the receptor binding activity of the central dopamine receptor agonist, ADTN.
AID61465Inhibitor constant of compound for low affinity component of [3H]spiroperidol/N-propylnorapomorphine binding to Dopamine receptor D2 in absence of Gpp(NH)p (pretreatment with 100 nM of compound)1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID1807005Positive allosteric modulation of human D2 receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP accumulation by measuring dopamine EC50 at 0.01 nM pretreated for 10 mins followed by forskolin stimulation for 5 mins and measu2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery of New Potent Positive Allosteric Modulators of Dopamine D
AID62474Inhibitory constant of compound in presence of Gpp(NH)p (Pre treated with 1 uM) calculated for the high affinity components of the [3H]spiroperidol binding to Dopamine receptor D21997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID62021Compound was evaluated for its ability to enhance the binding of the dopamine receptor agonist [3H]pramipexole to Dopamine receptor D2 at a concentration of 10E-9 M1998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Beta-analogs of PLG (L-prolyl-L-leucyl-glycinamide): ex-chiral pool syntheses and dopamine D2 receptor modulating effects.
AID62497Percentage of receptor in the high affinity form for the compound to Dopamine receptor D2 in absence of Gpp(NH)p1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID61466Inhibitor constant of compound for low affinity component of [3H]spiroperidol/N-propylnorapomorphine binding to Dopamine receptor D2 in presence of Gpp(NH)p1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID62300Enhancement of [3H]ADTN to dopamine receptors at concentration of 100 nM1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Dopamine receptor modulation by Pro-Leu-Gly-NH2 analogues possessing cyclic amino acid residues at the C-terminal position.
AID62471Inhibitory constant of compound in absence of Gpp(NH)p calculated for the low affinity components of the [3H]spiroperidol binding to Dopamine receptor D21997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID118946Ability to reverse electroconvulsive shock-induced amnesia in rodents following 0.1 mg/kg i.m. administration.1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Modified di- and tripeptides of the C-terminal portion of oxytocin and vasopressin as possible cognition activation agents.
AID735542Analgesic activity in Wistar rats assessed as increase in mechanical nociceptive threshold at 1 mg/kg, ip treated 20 mins after 1 mg/kg, ip noncompetitive opiate receptor antagonist, naloxone challenge measured after 15 to 30 mins by paw pressure test2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis of an MIF-1 analogue containing enantiopure (S)-α-trifluoromethyl-proline and biological evaluation on nociception.
AID735541Analgesic activity in Wistar rats assessed as increase in latency of response to pain at 1 mg/kg, ip treated 20 mins after 1 mg/kg, ip noncompetitive opiate receptor antagonist, naloxone challenge measured after 15 to 30 mins by hot plate test2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis of an MIF-1 analogue containing enantiopure (S)-α-trifluoromethyl-proline and biological evaluation on nociception.
AID1136080Suppression of oxotremorine-induced tremor in ICR mouse at 20 mg/kg, ip pretreated for 1 hr followed by oxotremorine-challenge1978Journal of medicinal chemistry, Feb, Volume: 21, Issue:2
Study of the structural requirements for dopa potentiation and oxotremorine antagonism by L-prolyl-L-leucylglycinamide.
AID61461Inhibitor constant of compound for high affinity component of [3H]spiroperidol/N-propylnorapomorphine binding to Dopamine receptor D2 in absence of Gpp(NH)p (pretreatment with 100 nM of compound)1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID1600455Agonist activity at human D2 receptor expressed in NIH/3T3 cells co-expressing beta-galactosidase assessed as increase in beta-galactosidase activity at 10 uM incubated for 5 days by spectrophotometry relative to control2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Applications of amide isosteres in medicinal chemistry.
AID774974Positive allosteric modulation of human dopamine D2S receptor expressed in CHO cell membranes assessed as stimulation of [3H]-NPA binding at 10'-12 to 10'-9 M after 60 mins by beta scintillation counting analysis2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis and allosteric modulation of the dopamine receptor by peptide analogs of L-prolyl-L-leucyl-glycinamide (PLG) modified in the L-proline or L-proline and L-leucine scaffolds.
AID184108Maximal increase in rotations at a dose of 1 mg/kg, ip in 6-hydroxydopamine-lesioned rat model of hemi-parkinsonism.1999Bioorganic & medicinal chemistry letters, Aug-16, Volume: 9, Issue:16
Synthesis and dopamine receptor modulating activity of unsubstituted and substituted triproline analogues of L-prolyl-L-leucyl-glycinamide (PLG).
AID62302Enhancement of [3H]ADTN to dopamine receptors at concentration of 10 nM1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Dopamine receptor modulation by Pro-Leu-Gly-NH2 analogues possessing cyclic amino acid residues at the C-terminal position.
AID62492Inhibitory constant of compound in presence of Gpp(NH)p (Pre treated with 1 uM) calculated for the low affinity components of the [3H]spiroperidol binding to Dopamine receptor D21997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID61462Inhibitor constant of compound for high affinity component of [3H]spiroperidol/N-propylnorapomorphine binding to Dopamine receptor D2 in presence of Gpp(NH)p1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID61469Percent of Dopamine receptor D2 in high affinity state for the compound in presence of Gpp(NH)p1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID62345Inhibitory constant of compound in absence of Gpp(NH)p (Pre treated with 1 uM) calculated for the high affinity components of the [3H]spiroperidol binding to Dopamine receptor D21997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID63986Inhibitor constant of compound for high affinity component of [3H]spiroperidol/N-propylnorapomorphine binding to Dopamine receptor D2 in absence of Gpp(NH)p1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID62476Inhibitory constant of compound in presence of Gpp(NH)p calculated for the high affinity components of the [3H]spiroperidol binding to Dopamine receptor D21997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID1136073Potentiation of dl-DOPA-induced behavioral effects in ICR mouse assessed as marked piloerection, profuse salivation, marked increased irritability and reactivity, jumping, squeaking and aggressive fighting at 10 mg/kg, ip administered 1 hr prior to dl-DOP1978Journal of medicinal chemistry, Feb, Volume: 21, Issue:2
Study of the structural requirements for dopa potentiation and oxotremorine antagonism by L-prolyl-L-leucylglycinamide.
AID62613Percentage of receptor in the low affinity form for the compound to Dopamine receptor D2 in absence of Gpp(NH)p1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID62482Percentage of receptor in the high affinity form for the compound to Dopamine receptor D2 in absence of Gpp(NH)p (pre treated with 1 uM)1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID191727Ability (% reversal in rats) to reverse electroconvulsive shock-induced amnesia in rodents at a dose of 0.10 (mg/kg) (following intramuscular dosing)1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Modified di- and tripeptides of the C-terminal portion of oxytocin and vasopressin as possible cognition activation agents.
AID226424Ratio of the high affinity state over low affinity state of dopamine D2 receptor in the presence of Gpp(NH)p.1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID226422Ratio of the high affinity state over low affinity state of dopamine D2 receptor in the absence of Gpp(NH)p.1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID61470Percent of Dopamine receptor D2 in high affinity state for the compound in presence of Gpp(NH)p (pretreatment with 100 nM of compound).1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID1807012Induction of morphological changes in human differentiated SH-SY5Y cells assessed as appearance of detached cells at 200 uM measured after 48 hrs by phase-contrast microscopic analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery of New Potent Positive Allosteric Modulators of Dopamine D
AID118943Ability to reverse electroconvulsive shock-induced amnesia in rodents following 1 ug/kg i.m. administration.1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Modified di- and tripeptides of the C-terminal portion of oxytocin and vasopressin as possible cognition activation agents.
AID1136078Suppression of oxotremorine-induced tremor in ICR mouse at 1 mg/kg, ip pretreated for 1 hr followed by oxotremorine-challenge1978Journal of medicinal chemistry, Feb, Volume: 21, Issue:2
Study of the structural requirements for dopa potentiation and oxotremorine antagonism by L-prolyl-L-leucylglycinamide.
AID191723Ability (% reversal in rats) to reverse electroconvulsive shock-induced amnesia in rodents at a dose of 0.010 (mg/kg) administered intramuscularly (im)1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Modified di- and tripeptides of the C-terminal portion of oxytocin and vasopressin as possible cognition activation agents.
AID61468Percent of Dopamine receptor D2 in high affinity state for the compound in absence of Gpp(NH)p (pretreatment with 100 nM of compound).1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID62607Inhibitory constant of compound in absence of Gpp(NH)p (Pre treated with 1 uM) calculated for the low affinity components of the [3H]spiroperidol binding to Dopamine receptor D21997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID62614Percentage of receptor in the low affinity form for the compound to Dopamine receptor D2 in absence of Gpp(NH)p (pre treated with 1 uM)1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID1136079Suppression of oxotremorine-induced tremor in ICR mouse at 4 mg/kg, ip pretreated for 1 hr followed by oxotremorine-challenge1978Journal of medicinal chemistry, Feb, Volume: 21, Issue:2
Study of the structural requirements for dopa potentiation and oxotremorine antagonism by L-prolyl-L-leucylglycinamide.
AID118944Ability to reverse electroconvulsive shock-induced amnesia in rodents following 0.01 mg/kg i.m. administration.1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Modified di- and tripeptides of the C-terminal portion of oxytocin and vasopressin as possible cognition activation agents.
AID62498Percentage of receptor in the high affinity form for the compound to Dopamine receptor D2 in presence of Gpp(NH)p1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.
AID1136072Potentiation of dl-DOPA-induced behavioral effects in ICR mouse assessed as marked piloerection, profuse salivation, marked increased irritability and reactivity, jumping, squeaking and aggressive fighting at 1 mg/kg, ip administered 1 hr prior to dl-DOPA1978Journal of medicinal chemistry, Feb, Volume: 21, Issue:2
Study of the structural requirements for dopa potentiation and oxotremorine antagonism by L-prolyl-L-leucylglycinamide.
AID61474Percent of Dopamine receptor D2 in low affinity state for the compound in presence of Gpp(NH)p (pretreatment with 100 nM of compound).1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID191721Ability (% reversal in rats) to reverse electroconvulsive shock-induced amnesia in rodents at a dose of 0.0010 (mg/kg) (following i.m. administration)1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Modified di- and tripeptides of the C-terminal portion of oxytocin and vasopressin as possible cognition activation agents.
AID61464Inhibitor constant of compound for low affinity component of [3H]spiroperidol/N-propylnorapomorphine binding to Dopamine receptor D2 in absence of Gpp(NH)p1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.
AID1807006Positive allosteric modulation of human D2 receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP accumulation by measuring dopamine Emax at 0.01 nM pretreated for 10 mins followed by forskolin stimulation for 5 mins and measu2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery of New Potent Positive Allosteric Modulators of Dopamine D
AID735540Analgesic activity in Wistar rats assessed as increase in mechanical nociceptive threshold at 1 mg/kg, ip treated 20 mins after 10 mg/kg, ip NOS inhibitor, L-NAME challenge measured after 15 to 45 mins by paw pressure test2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis of an MIF-1 analogue containing enantiopure (S)-α-trifluoromethyl-proline and biological evaluation on nociception.
AID282083Activity at human dopamine D2 receptor in NIH/3T3 cells assessed as enhancement of NPA-stimulated beta-galactosidase activity at 10 nM after 5 days by R-SAT assay2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Design, synthesis and evaluation of a PLG tripeptidomimetic based on a pyridine scaffold.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (21)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (23.81)18.7374
1990's8 (38.10)18.2507
2000's3 (14.29)29.6817
2010's4 (19.05)24.3611
2020's1 (4.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.64

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

MetricThis Compound (vs All)
Research Demand Index20.64 (24.57)
Research Supply Index3.09 (2.92)
Research Growth Index4.66 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.64)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (9.52%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other19 (90.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]