Page last updated: 2024-12-11
tabimorelin
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
tabimorelin: a growth hormone secretagogue; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 9810101 |
| CHEMBL ID | 281764 |
| SCHEMBL ID | 209441 |
| MeSH ID | M0331930 |
Synonyms (25)
| Synonym |
|---|
| NCGC00092365-01 |
| nnc-26-0703 |
| nn-703 |
| nn703 |
| CHEMBL281764 , |
| tabimorelin |
| (e)-5-amino-n,5-dimethyl-n-((r)-1-(methyl((r)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl)amino)-3-(naphthalen-2-yl)-1-oxopropan-2-yl)hex-2-enamide |
| bdbm50066816 |
| (e)-5-amino-5-methyl-hex-2-enoic acid methyl-{(r)-1-[methyl-((r)-1-methylcarbamoyl-2-phenyl-ethyl)-carbamoyl]-2-naphthalen-2-yl-ethyl}-amide |
| (e)-2-methyl-6-(methyl((r)-1-(methyl((r)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl)amino)-3-(naphthalen-2-yl)-1-oxopropan-2-yl)amino)-6-oxohex-4-en-2-aminium |
| nn 703 |
| 193079-69-5 |
| (r)-alpha-((e)-5-amino-n,5-dimethyl-2-hexenamido)-n-methyl-n-((r)-alpha-(methylcarbamoyl)phenethyl)-2-naphthalenepropionamide |
| unii-l51cbe03kf |
| tabimorelin [inn] |
| l51cbe03kf , |
| d-phenylalaninamide, n-((2e)-5-amino-5-methyl-1-oxo-2-hexen-1-yl)-n-methyl-3-(2-naphthalenyl)-d-alanyl-n,n.alpha.-dimethyl- |
| tabimorelin [who-dd] |
| 249762-09-2 |
| SCHEMBL209441 |
| (2e)-5-amino-5-methylhex-2-enoic acid n-methyl-n-((1r)-1-(n-methyl-n-((1r)-1-(methylcarbamoyl)-2-phenylethyl)carbamoyl)-2-(2-naphthyl)ethyl)amide |
| WURGZWOTGMLDJP-ZCYANPAGSA-N |
| Q7673066 |
| (e)-5-amino-n,5-dimethyl-n-[(2r)-1-[methyl-[(2r)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl]amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]hex-2-enamide |
| DTXSID601027158 |
Research Excerpts
Treatment
Tabimorelin treatment induced hyperphagia and adiposity (increased total fat mass and gain in body weight) in lean control rats. These parameters were not increased in ZDF rats. Treatment with tabimorelin increased hypothalamic mRNA expression of the anabolic neuropeptide Y (NPY) mRNA.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Tabimorelin treatment induced hyperphagia and adiposity (increased total fat mass and gain in body weight) in lean control rats, while these parameters were not increased in ZDF rats. " | ( Adipogenic and orexigenic effects of the ghrelin-receptor ligand tabimorelin are diminished in leptin-signalling-deficient ZDF rats. Ahnfelt-Rønne, I; Holm, AM; Johansen, PB; Rømer, J, 2004) | 2 |
| "Treatment with tabimorelin of lean control rats increased hypothalamic mRNA expression of the anabolic neuropeptide Y (NPY) mRNA and decreased hypothalamic expression of the catabolic peptide pro-opiomelanocortin (POMC) mRNA." | ( Adipogenic and orexigenic effects of the ghrelin-receptor ligand tabimorelin are diminished in leptin-signalling-deficient ZDF rats. Ahnfelt-Rønne, I; Holm, AM; Johansen, PB; Rømer, J, 2004) | 0.9 |
Bioavailability
Dosage Studied
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (24)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 39.8107 | 0.0251 | 20.2376 | 39.8107 | AID893 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 39.8107 | 0.0251 | 20.2376 | 39.8107 | AID893 |
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 25.1189 | 0.0126 | 10.6917 | 88.5700 | AID887 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 7.9433 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 19.9526 | 0.3162 | 12.7657 | 31.6228 | AID881 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 19.9526 | 0.0063 | 8.2350 | 39.8107 | AID881 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Growth hormone secretagogue receptor type 1 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0180 | 0.0013 | 0.0154 | 0.0600 | AID195900 |
| Growth hormone secretagogue receptor type 1 | Homo sapiens (human) | EC50 (µMol) | 0.0030 | 0.0002 | 0.0087 | 0.0660 | AID265201; AID306735 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (68)
Molecular Functions (12)
Ceullar Components (15)
Bioassays (5)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID195905 | Tested for GH-releasing property using classical rat pituitary cell assay | 1998 | Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19 | Novel orally active growth hormone secretagogues. |
| AID306735 | Agonist activity at human GHS-R1 | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Modeling of human ghrelin receptor (hGHS-R1a) in its close state and validation by molecular docking. |
| AID265201 | Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH release | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11 | Construction of human ghrelin receptor (hGHS-R1a) model using a fragmental prediction approach and validation through docking analysis. |
| AID195900 | Tested for GH-releasing property using classical rat pituitary cell assay | 1998 | Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19 | Novel orally active growth hormone secretagogues. |
| AID175498 | Compound was tested in vitro for growth hormone release in rat pituitary model | 1999 | Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9 | New growth hormone secretagogues: C-terminal modified sulfonamide-analogues of NN703. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (21)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 3 (14.29) | 18.2507 |
| 2000's | 17 (80.95) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 1 (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: 20.48
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.
| This Compound (20.48) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 6 (28.57%) | 5.53% |
| Reviews | 1 (4.76%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 14 (66.67%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||