Page last updated: 2024-10-15

galantide

Description

galantide: consists of 20-amino acid residues, 12 AA from the N-terminal of galanin and the C-terminal part of Substance P; blocks the galanin-mediated inhibition of glucose-induced insulin secretion; amino acid sequence given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID16132126
CHEMBL ID526003
MeSH IDM0202197

Synonyms (14)

Synonym
galanin (1-12)-pro-substance p (5-11)
l-methioninamide, glycyl-l-tryptophyl-l-threonyl-l-leucyl-l-asparaginyl-l-seryl-l-alanylglycyl-l-tyrosyl-l-leucyl-l-leucylglycyl-l-prolyl-l-glutaminyl-l-glutaminyl-l-phenylalanyl-l-phenylalanylglycyl-l-leucyl-
138579-66-5
galantide
galanin (1-13)-sp-(5-11)
bdbm50273369
gwtlnsagyllgpqqffglm-conh2
CHEMBL526003 ,
galantide, >=90% (hplc)
mfcd00144384
galanin (1-13)-substance p (5-11) amide
DTXSID00160714
l-methioninamide,glycyl-l-tryptophyl-l-threonyl-l-leucyl-l-asparaginyl-l-seryl-l-alanylglycyl-l-tyrosyl-l-leucyl-l-leucylglycyl-l-prolyl-l-glutaminyl-l-glutaminyl-l-phenylalanyl-l-phenylalanylglycyl-l
AKOS040741780

Effects

ExcerptReference
"Galantide has been shown to be a novel high affinity antagonist to galanin, since it inhibits galanin-mediated inhibition of glucose-induced insulin secretion and the neuronal action of galanin in the brain."( Modulation of neurotransmission in guinea-pig airways by galanin and the effect of a new antagonist galantide.
Barnes, PJ; Belvisi, MG; Takahashi, T, 1994
)

Actions

ExcerptReference
"Galantide did not activate the K+ conductance but produced a concentration-dependent antagonism (IC50 = 4 nM) of the galanin-induced increase in K+ conductance."( Galantide distinguishes putative subtypes of galanin receptors in mudpuppy parasympathetic neurons.
Merriam, LA; Mulvaney, JM; Parsons, RL, 1995
)

Treatment

ExcerptReference
"Treatment with galantide alone ameliorated most of the indices of AP studied, whereas treatment with octreotide reduced pancreatic MPO activity and acinar cell damage. "( Octreotide negates the benefit of galantide when used in the treatment of caerulein-induced acute pancreatitis in mice.
Barreto, SG; Carati, CJ; Saccone, GT; Schloithe, AC; Toouli, J, 2010
)

Pharmacokinetics

ExcerptReference
" This study aimed to develop a semi-mechanistic population pharmacokinetic (PopPK) model to characterize the pharmacokinetic (PK) profile of M15-2, the active metabolite of vicagrel and clopidogrel, and to evaluate the influence of CYP2C19 polymorphisms and other covariates in healthy subjects and patients with acute coronary syndrome (ACS) after oral administration."( Semi-mechanistic population pharmacokinetics analysis reveals distinct CYP2C19 dependency in the bioactivation of vicagrel and clopidogrel to active metabolite M15-2.
Gong, Y; He, Y; Lai, X; Li, YG; Liu, X; Liu, Y; Sun, H; Yan, X; Zhang, EY; Zhang, L, 2022
)

Dosage Studied

ExcerptReference
" Advantages in both PK and pharmacogenetics suggest that vicagrel may reduce the complexity of currently recommended CYP2C19-based dosage adjustment for clopidogrel."( Semi-mechanistic population pharmacokinetics analysis reveals distinct CYP2C19 dependency in the bioactivation of vicagrel and clopidogrel to active metabolite M15-2.
Gong, Y; He, Y; Lai, X; Li, YG; Liu, X; Liu, Y; Sun, H; Yan, X; Zhang, EY; Zhang, L, 2022
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Galanin receptor type 2Homo sapiens (human)Ki0.00110.00110.00150.0018AID459287
Galanin receptor type 1Homo sapiens (human)Ki0.00000.00000.00000.0001AID459286
[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)
Galanin receptor type 2Homo sapiens (human)Kd0.00100.00100.00270.0050AID413941
Galanin receptor type 3Homo sapiens (human)Kd0.04000.01500.12330.3150AID413942
Galanin receptor type 1Homo sapiens (human)Kd0.00030.00010.00120.0032AID413940
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (19)

Processvia Protein(s)Taxonomy
muscle contractionGalanin receptor type 2Homo sapiens (human)
cell surface receptor signaling pathwayGalanin receptor type 2Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayGalanin receptor type 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayGalanin receptor type 2Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationGalanin receptor type 2Homo sapiens (human)
learning or memoryGalanin receptor type 2Homo sapiens (human)
feeding behaviorGalanin receptor type 2Homo sapiens (human)
neuron projection developmentGalanin receptor type 2Homo sapiens (human)
inositol phosphate metabolic processGalanin receptor type 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIGalanin receptor type 2Homo sapiens (human)
phosphatidylinositol metabolic processGalanin receptor type 2Homo sapiens (human)
galanin-activated signaling pathwayGalanin receptor type 2Homo sapiens (human)
positive regulation of large conductance calcium-activated potassium channel activityGalanin receptor type 2Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayGalanin receptor type 2Homo sapiens (human)
neuropeptide signaling pathwayGalanin receptor type 2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerGalanin receptor type 3Homo sapiens (human)
chemical synaptic transmissionGalanin receptor type 3Homo sapiens (human)
learning or memoryGalanin receptor type 3Homo sapiens (human)
feeding behaviorGalanin receptor type 3Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIGalanin receptor type 3Homo sapiens (human)
galanin-activated signaling pathwayGalanin receptor type 3Homo sapiens (human)
neuropeptide signaling pathwayGalanin receptor type 3Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayGalanin receptor type 3Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayGalanin receptor type 1Homo sapiens (human)
negative regulation of adenylate cyclase activityGalanin receptor type 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationGalanin receptor type 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIGalanin receptor type 1Homo sapiens (human)
positive regulation of cortisol secretionGalanin receptor type 1Homo sapiens (human)
neuropeptide signaling pathwayGalanin receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
galanin receptor activityGalanin receptor type 2Homo sapiens (human)
protein bindingGalanin receptor type 2Homo sapiens (human)
peptide hormone bindingGalanin receptor type 2Homo sapiens (human)
neuropeptide bindingGalanin receptor type 2Homo sapiens (human)
galanin receptor activityGalanin receptor type 3Homo sapiens (human)
peptide hormone bindingGalanin receptor type 3Homo sapiens (human)
galanin receptor activityGalanin receptor type 1Homo sapiens (human)
protein bindingGalanin receptor type 1Homo sapiens (human)
peptide hormone bindingGalanin receptor type 1Homo sapiens (human)
neuropeptide bindingGalanin receptor type 1Homo sapiens (human)
G protein-coupled peptide receptor activityGalanin receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
plasma membraneGalanin receptor type 2Homo sapiens (human)
ciliumGalanin receptor type 2Homo sapiens (human)
membraneGalanin receptor type 2Homo sapiens (human)
plasma membraneGalanin receptor type 2Homo sapiens (human)
plasma membraneGalanin receptor type 3Homo sapiens (human)
ciliumGalanin receptor type 3Homo sapiens (human)
membraneGalanin receptor type 3Homo sapiens (human)
synapseGalanin receptor type 3Homo sapiens (human)
non-motile ciliumGalanin receptor type 3Homo sapiens (human)
plasma membraneGalanin receptor type 3Homo sapiens (human)
plasma membraneGalanin receptor type 1Homo sapiens (human)
membraneGalanin receptor type 1Homo sapiens (human)
plasma membraneGalanin receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID459287Binding affinity to human GalR22010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.
AID413941Binding affinity to human GalR22008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Design, synthesis, and characterization of high-affinity, systemically-active galanin analogues with potent anticonvulsant activities.
AID459286Binding affinity to human GalR12010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.
AID413940Binding affinity to human GalR12008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Design, synthesis, and characterization of high-affinity, systemically-active galanin analogues with potent anticonvulsant activities.
AID413942Binding affinity to human GalR32008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Design, synthesis, and characterization of high-affinity, systemically-active galanin analogues with potent anticonvulsant activities.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (78)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's38 (48.72)18.2507
2000's20 (25.64)29.6817
2010's14 (17.95)24.3611
2020's6 (7.69)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies1 (1.22%)4.05%
Observational0 (0.00%)0.25%
Other81 (98.78%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]