Compounds > bremelanotide
Page last updated: 2024-11-12

bremelanotide

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Description

bremelanotide: a synthetic peptide analogue of alpha-MSH, is an agonist at melanocortin receptors including the MC3R and MC4R, which are expressed primarily in the central nervous system; [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9941379
CHEMBL ID2070241
CHEBI ID177849
SCHEMBL ID13574795
SCHEMBL ID20337333
MeSH IDM0500526

Synonyms (40)

Synonym
bremelanotide
(3s,6s,9r,12s,15s,23s)-15-[[(2s)-2-acetamidohexanoyl]amino]-9-benzyl-6-[3-(diaminomethylideneamino)propyl]-12-(1h-imidazol-5-ylmethyl)-3-(1h-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-23-carboxylic acid
CHEBI:177849
D06569
pt-141
bremelanotide (usan/inn)
AKOS005145807
unii-6y24o4f92s
n-acetyl-l-2-aminohexanoyl-l-alpha-aspartyl-l-histidyl-d-phenylalanyl-l-arginyl-l-tryptophyl-l-lysine-(2->7)-lactam
l-lysine, n-acetyl-l-norleucyl-l-alpha-aspartyl-l-histidyl-d-phenylalanyl-l-arginyl-l-tryptophyl-, (2->7)-lactam
6y24o4f92s ,
bremelanotide [usan:inn]
bdbm50389769
pt-141 free base
CHEMBL2070241
bremelanotide, pt-141
HS-2024
SCHEMBL13574795
Q-200747
bremelanotide [mi]
l-lysine, n-acetyl-l-norleucyl-l-.alpha.-aspartyl-l-histidyl-d-phenylalanyl-l-arginyl-l-tryptophyl-, (2->7)-lactam
bremelanotide [usan]
n-acetyl-l-2-aminohexanoyl-l-.alpha.-aspartyl-l-histidyl-d-phenylalanyl-l-arginyl-l-tryptophyl-l-lysine-(2->7)-lactam
bremelanotide [who-dd]
bremelanotide [inn]
SCHEMBL20337333
gtpl10408
pt141
(1z,3s,4z,6s,7z,9r,10e,12s,13z,15s,17e,23s)-12-((1h-imidazol-5-yl)methyl)-3-((1h-indol-3-yl)methyl)-9-benzyl-6-(3-guanidinopropyl)-2,5,8,11,14,17-hexahydroxy-15-(((s,z)-1-hydroxy-2-(((z)-1-hydroxyethylidene)amino)hexylidene)amino)-1,4,7,10,13,18-hexaazacy
DB11653
DTXSID40893711 ,
Q415353
189691-06-3 (free base)
(3s,6s,9r,12s,15s,23s)-12-((1h-imidazol-5-yl)methyl)-3-((1h-indol-3-yl)methyl)-15-((s)-2-acetamidohexanamido)-9-benzyl-6-(3-guanidinopropyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexaazacyclotricosane-23-carboxylic acid
pt-141 (bremelanotide)
CS-0013839
HY-18678
bremelanotida
bremelanotidum
dtxcid701323799

Research Excerpts

Overview

Bremelanotide (Vyleesi™) is a melanocortin receptor agonist recently approved in the USA for the treatment of premenopausal women with acquired, generalized hypoactive sexual desire disorder. The MCR agonist nonselectively activates several of the receptor subtypes, of which subtype 4 (MC4R) is the most relevant at therapeutic doses.

ExcerptReferenceRelevance
"Bremelanotide (Vyleesi™) is a melanocortin receptor agonist recently approved in the USA for the treatment of premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD), as characterized by low sexual desire that causes marked distress or interpersonal difficulty. "( Bremelanotide: First Approval.
Dhillon, S; Keam, SJ, 2019)		3.4
"Bremelanotide is an MCR agonist that nonselectively activates several of the receptor subtypes, of which subtype 4 (MC4R) is the most relevant at therapeutic doses."( The neurobiology of bremelanotide for the treatment of hypoactive sexual desire disorder in premenopausal women.
Clayton, AH; Pfaus, JG; Sadiq, A; Spana, C, 2022)		1.77
"Bremelanotide is an on-demand, subcutaneous melanocortin-receptor agonist that binds to the melanocortin receptor 4 and is being developed for the treatment of female sexual dysfunction."( Usefulness of ambulatory blood pressure monitoring to assess the melanocortin receptor agonist bremelanotide.
Jordan, R; Lucas, J; Myers, MG; White, WB, 2017)		1.4
"Bremelanotide is a synthetic peptide melanocortin analog of alpha-melanocyte-stimulating hormone that is an agonist at melanocortin receptors MC3R and MC4R."( An effect on the subjective sexual response in premenopausal women with sexual arousal disorder by bremelanotide (PT-141), a melanocortin receptor agonist.
Diamond, LE; Earle, DC; Harning, R; Heiman, JR; Perelman, MA; Rosen, RC, 2006)		1.27
"Bremelanotide is an analogue of the naturally occurring peptide alpha-melanocyte-stimulating hormone (alpha-MSH). "( Bremelanotide: an overview of preclinical CNS effects on female sexual function.
Gelez, H; Giuliano, F; Pfaus, J, 2007)		3.23

Toxicity

ExcerptReferenceRelevance
" Flushing and nausea were the most common adverse events reported in both studies and no clinically significant changes in vital signs, laboratory tests, ECGs, or physical exams were observed."( Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction.
Diamond, LE; Earle, DC; Molinoff, PB; Rosen, RC; Willett, MS, 2004)		0.32
" PT-141 was safe and well tolerated in both studies."( Evaluation of the safety, pharmacokinetics and pharmacodynamic effects of subcutaneously administered PT-141, a melanocortin receptor agonist, in healthy male subjects and in patients with an inadequate response to Viagra.
Diamond, LE; Earle, DC; Molinoff, PB; Rosen, RC; Shadiack, AM, 2004)		0.32
" Vital signs, self-rated sedation scores, nursing and medical observations, and spontaneous reporting by participants provided the basis for evaluation of adverse events."( Phase I Randomized Placebo-controlled, Double-blind Study of the Safety and Tolerability of Bremelanotide Coadministered With Ethanol in Healthy Male and Female Participants.
Clayton, AH; DeRogatis, LR; Jordan, R; Lucas, J, 2017)		0.68
"6 g/kg ethanol, were found to be safe and generally well tolerated with mean maximum ethanol concentrations exceeding 80 mg/dL in women."( Phase I Randomized Placebo-controlled, Double-blind Study of the Safety and Tolerability of Bremelanotide Coadministered With Ethanol in Healthy Male and Female Participants.
Clayton, AH; DeRogatis, LR; Jordan, R; Lucas, J, 2017)		0.68
" The results of this Phase I study found that BMT and ethanol can be safely coadministered and are generally well tolerated with no reports of drug-related serious adverse events."( Phase I Randomized Placebo-controlled, Double-blind Study of the Safety and Tolerability of Bremelanotide Coadministered With Ethanol in Healthy Male and Female Participants.
Clayton, AH; DeRogatis, LR; Jordan, R; Lucas, J, 2017)		0.68
"Women who completed the 24-week double-blind core phase of RECONNECT, composed of two parallel phase 3 trials (301 and 302) examining the safety and efficacy of bremelanotide compared with placebo in premenopausal women with hypoactive sexual desire disorder, could enroll in the 52-week open-label extension, provided they had not experienced serious adverse events during the core phase."( Long-Term Safety and Efficacy of Bremelanotide for Hypoactive Sexual Desire Disorder.
Clayton, AH; Jordan, R; Kingsberg, SA; Krop, J; Lucas, J; Portman, D; Simon, JA; Williams, LA, 2019)		0.99
" The most common treatment-emergent adverse events considered related to study drug were nausea (40."( Long-Term Safety and Efficacy of Bremelanotide for Hypoactive Sexual Desire Disorder.
Clayton, AH; Jordan, R; Kingsberg, SA; Krop, J; Lucas, J; Portman, D; Simon, JA; Williams, LA, 2019)		0.8

Bioavailability

ExcerptReferenceRelevance
"Ultrastable cyclic peptide frameworks offer great potential for drug design due to their improved bioavailability compared to their linear analogues."( Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
Ahmad Fuaad, A; Bauer, U; Cai, M; Cheneval, O; Craik, DJ; Cromm, PM; Daly, NL; Dellsén, A; Durek, T; Harvey, PJ; Hruby, VJ; Kaas, Q; Kessler, H; Knerr, L; Larsson, N; Österlund, T; Plowright, AT; Schroeder, CI; Weidmann, J; White, AM; Zhou, Y, 2018)		0.48
[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)
Melanocortin receptor 4Homo sapiens (human)Ki0.01670.00000.30864.8860AID1480165; AID1812562; AID1852336; AID677161
Melanocortin receptor 5Homo sapiens (human)IC50 (µMol)0.19800.00091.25669.5180AID1480166; AID1812563; AID1852340
Melanocortin receptor 5Homo sapiens (human)Ki0.01700.00053.52658.9290AID677160
Melanocortin receptor 3Homo sapiens (human)Ki0.16070.00010.24522.8650AID1480164; AID1812561; AID1852335; AID677159
Melanocyte-stimulating hormone receptorHomo sapiens (human)Ki0.00300.00000.00650.0370AID1480163; AID1812560; AID1852334; AID677158
[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)
Melanocortin receptor 4Homo sapiens (human)EC50 (µMol)0.00130.00000.09112.6000AID1480174; AID1480175; AID1812559; AID1812567; AID1852339; AID677162
Melanocortin receptor 3Homo sapiens (human)EC50 (µMol)0.00130.00010.01270.2480AID1480173; AID1812558; AID1852338
Melanocyte-stimulating hormone receptorHomo sapiens (human)EC50 (µMol)0.00010.00000.00800.2280AID1480172; AID1812557; AID1852337
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (33)

Processvia Protein(s)Taxonomy
diet induced thermogenesisMelanocortin receptor 4Homo sapiens (human)
energy reserve metabolic processMelanocortin receptor 4Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMelanocortin receptor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 4Homo sapiens (human)
feeding behaviorMelanocortin receptor 4Homo sapiens (human)
insulin secretionMelanocortin receptor 4Homo sapiens (human)
response to insulinMelanocortin receptor 4Homo sapiens (human)
positive regulation of bone resorptionMelanocortin receptor 4Homo sapiens (human)
regulation of eating behaviorMelanocortin receptor 4Homo sapiens (human)
response to melanocyte-stimulating hormoneMelanocortin receptor 4Homo sapiens (human)
negative regulation of feeding behaviorMelanocortin receptor 4Homo sapiens (human)
regulation of grooming behaviorMelanocortin receptor 4Homo sapiens (human)
regulation of metabolic processMelanocortin receptor 4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelanocortin receptor 5Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 5Homo sapiens (human)
regulation of metabolic processMelanocortin receptor 5Homo sapiens (human)
regulation of heart rateMelanocortin receptor 3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelanocortin receptor 3Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 3Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 3Homo sapiens (human)
regulation of blood pressureMelanocortin receptor 3Homo sapiens (human)
circadian regulation of gene expressionMelanocortin receptor 3Homo sapiens (human)
homoiothermyMelanocortin receptor 3Homo sapiens (human)
locomotor rhythmMelanocortin receptor 3Homo sapiens (human)
sodium ion homeostasisMelanocortin receptor 3Homo sapiens (human)
regulation of feeding behaviorMelanocortin receptor 3Homo sapiens (human)
regulation of metabolic processMelanocortin receptor 3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelanocyte-stimulating hormone receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocyte-stimulating hormone receptorHomo sapiens (human)
UV protectionMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of protein kinase A signalingMelanocyte-stimulating hormone receptorHomo sapiens (human)
sensory perception of painMelanocyte-stimulating hormone receptorHomo sapiens (human)
negative regulation of tumor necrosis factor productionMelanocyte-stimulating hormone receptorHomo sapiens (human)
intracellular signal transductionMelanocyte-stimulating hormone receptorHomo sapiens (human)
melanin biosynthetic processMelanocyte-stimulating hormone receptorHomo sapiens (human)
pigmentationMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIMelanocyte-stimulating hormone receptorHomo sapiens (human)
UV-damage excision repairMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of protein kinase C signalingMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of feeding behaviorMelanocyte-stimulating hormone receptorHomo sapiens (human)
regulation of metabolic processMelanocyte-stimulating hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
melanocortin receptor activityMelanocortin receptor 4Homo sapiens (human)
melanocyte-stimulating hormone receptor activityMelanocortin receptor 4Homo sapiens (human)
protein bindingMelanocortin receptor 4Homo sapiens (human)
peptide hormone bindingMelanocortin receptor 4Homo sapiens (human)
ubiquitin protein ligase bindingMelanocortin receptor 4Homo sapiens (human)
neuropeptide bindingMelanocortin receptor 4Homo sapiens (human)
protein bindingMelanocortin receptor 5Homo sapiens (human)
hormone bindingMelanocortin receptor 5Homo sapiens (human)
melanocortin receptor activityMelanocortin receptor 5Homo sapiens (human)
melanocortin receptor activityMelanocortin receptor 3Homo sapiens (human)
melanocyte-stimulating hormone receptor activityMelanocortin receptor 3Homo sapiens (human)
protein bindingMelanocortin receptor 3Homo sapiens (human)
neuropeptide bindingMelanocortin receptor 3Homo sapiens (human)
peptide hormone bindingMelanocortin receptor 3Homo sapiens (human)
melanocortin receptor activityMelanocyte-stimulating hormone receptorHomo sapiens (human)
melanocyte-stimulating hormone receptor activityMelanocyte-stimulating hormone receptorHomo sapiens (human)
protein bindingMelanocyte-stimulating hormone receptorHomo sapiens (human)
G protein-coupled peptide receptor activityMelanocyte-stimulating hormone receptorHomo sapiens (human)
ubiquitin protein ligase bindingMelanocyte-stimulating hormone receptorHomo sapiens (human)
hormone bindingMelanocyte-stimulating hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
plasma membraneMelanocortin receptor 4Homo sapiens (human)
membraneMelanocortin receptor 4Homo sapiens (human)
plasma membraneMelanocortin receptor 4Homo sapiens (human)
cytoplasmMelanocortin receptor 4Homo sapiens (human)
plasma membraneMelanocortin receptor 5Homo sapiens (human)
plasma membraneMelanocortin receptor 5Homo sapiens (human)
cytoplasmMelanocortin receptor 5Homo sapiens (human)
plasma membraneMelanocortin receptor 3Homo sapiens (human)
cytoplasmMelanocortin receptor 3Homo sapiens (human)
plasma membraneMelanocortin receptor 3Homo sapiens (human)
plasma membraneMelanocyte-stimulating hormone receptorHomo sapiens (human)
plasma membraneMelanocyte-stimulating hormone receptorHomo sapiens (human)
cytoplasmMelanocyte-stimulating hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (36)

Assay IDTitleYearJournalArticle
AID1852334Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1852342Selectivity ratio of Ki for human MC4R to Ki for human MC1R2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1480173Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
AID1812563Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1852344Selectivity ratio of EC50 for human MC4R to EC50 for human MC1R2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1480175Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
AID677164Antiobesity activity in Sprague-Dawley rat assessed as reduction of food intake at 3 mg/kg, sc qd measured after 7 to 24 hrs relative to control2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID677163Antiobesity activity in Sprague-Dawley rat assessed as reduction of food intake at 3 mg/kg, sc qd measured up to 7 hrs relative to control2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID677162Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID1812560Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1812567Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID677168Half life in human2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID1812558Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1852340Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1852339Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID677158Displacement of [125I]-NAD-alpha-MSH from human recombinant MC1 receptor expressed in BHK570 cells after 90 mins in presence of ovalbumin2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID1480166Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
AID677161Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID677165Antiobesity activity in Sprague-Dawley rat assessed as reduction of food intake at 3 mg/kg, sc qd measured after 24 to 48 hrs relative to control2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID1812562Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1812561Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1852338Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1852337Agonist activity at human MC1R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1852343Selectivity ratio of EC50 for human MC3R to EC50 for human MC1R2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1480163Displacement of [125I]-NDP-alpha-MSH from human MC1R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
AID1852341Selectivity ratio of Ki for human MC3R to Ki for human MC1R2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID677159Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID677160Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID1480164Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
AID1812557Agonist activity at human melanocortin receptor 1 expressed in human T-Rex-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1480174Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
AID1812559Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1480165Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
AID1852335Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1852336Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1480172Agonist activity at human MC1R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (44)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's14 (31.82)29.6817
2010's18 (40.91)24.3611
2020's12 (27.27)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 (%)
Trials14 (29.79%)5.53%
Reviews15 (31.91%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other18 (38.30%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
bupropion
Bupropion: A propiophenone-derived antidepressant and antismoking agent that inhibits the uptake of DOPAMINE.. bupropion : An aromatic ketone that is propiophenone carrying a tert-butylamino group at position 2 and a chloro substituent at position 3 on the phenyl ring.		3.1810aromatic ketone;
monochlorobenzenes;
secondary amino compound		antidepressant;
environmental contaminant;
xenobiotic
amifampridine
Amifampridine: 4-Aminopyridine derivative that acts as a POTASSIUM CHANNEL blocker to increase release of ACETYLCHOLINE from nerve terminals. It is used in the treatment of CONGENITAL MYASTHENIC SYNDROMES.		2.2510aminopyridine
apomorphine
Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.		4.0620aporphine alkaloidalpha-adrenergic drug;
antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
emetic;
serotonergic drug
melanotan-ii
melanotan-II: synthetic cyclic heptapeptide, an analog of alpha-melanotropin (4,10); capable of stimulating melanin synthesis & promoting rapid tanning of skin; currently in trials for use in the prevention of sunlight-induced skin cancer		3.240organic molecular entity
mdl 100907
Serotonin 5-HT2 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.		3.6220
flibanserin
[no description available]		10.1850benzimidazoles;
N-alkylpiperazine;
N-arylpiperazine;
organofluorine compound		antidepressant;
serotonergic agonist;
serotonergic antagonist
rm-493
setmelanotide: an anti-obesity agent		2.7620
rifamycins
[no description available]		2.2510
alpha-msh
[no description available]		2.0710peptide hormoneanti-inflammatory agent
msh, 4-nle-7-phe-alpha-
[no description available]		2.0710polypeptidedermatologic drug
bc-3781
[no description available]		2.2510
siponimod
siponimod: S1P receptor modulator		2.2510
sildenafil citrate
Sildenafil Citrate: A PHOSPHODIESTERASE TYPE-5 INHIBITOR; VASODILATOR AGENT and UROLOGICAL AGENT that is used in the treatment of ERECTILE DYSFUNCTION and PRIMARY PULMONARY HYPERTENSION.. sildenafil citrate : The citrate salt of sildenafil.		6.3543citrate saltEC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
ConditionIndicatedRelationship StrengthStudiesTrials
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		07.4110
Obesity
A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).		02.4110
Frigidity
[description not available]		015.063718
Sexual Dysfunctions, Psychological
Disturbances in sexual desire and the psychophysiologic changes that characterize the sexual response cycle and cause marked distress and interpersonal difficulty. (APA, DSM-IV, 1994)		015.063718
Nausea
An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.		17.131
Adverse Effects, Long Term
[description not available]		05.0740
Central Hypothyroidism
[description not available]		02.1510
Hypothyroidism
A syndrome that results from abnormally low secretion of THYROID HORMONES from the THYROID GLAND, leading to a decrease in BASAL METABOLIC RATE. In its most severe form, there is accumulation of MUCOPOLYSACCHARIDES in the SKIN and EDEMA, known as MYXEDEMA. It may be primary or secondary due to other pituitary disease, or hypothalamic dysfunction.		02.1510
Sex Disorders
[description not available]		08.4284
Sexual Dysfunction, Physiological
Physiological disturbances in normal sexual performance in either the male or the female.		110.4284
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		03.1210
Impotence
[description not available]		08.0185
Erectile Dysfunction
The inability in the male to have a PENILE ERECTION due to psychological or organ dysfunction.		08.0185
Bilateral Headache
[description not available]		03.411
Emesis
[description not available]		03.411
Headache
The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS.		03.411
Vomiting
The forcible expulsion of the contents of the STOMACH through the MOUTH.		03.411
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		03.3520