PD 168368: a neuromedin B receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 9937534 |
| CHEMBL ID | 329650 |
| SCHEMBL ID | 6249801 |
| MeSH ID | M0378152 |
| Synonym |
|---|
| CHEMBL329650 , |
| (2s)-3-(1h-indol-3-yl)-2-methyl-2-[(4-nitrophenyl)carbamoylamino]-n-[(1-pyridin-2-ylcyclohexyl)methyl]propanamide |
| pd 168368 |
| pd-168368 |
| pd168368 , |
| gtpl621 |
| (s)-3-(1h-indol-3-yl)-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-n-(1-pyridin-2-yl-cyclohexylmethyl)-propionamide |
| bdbm50071735 |
| (s)-a-methyl-a-[[[(4-nitrophenyl)amino]carbonyl]amino]-n-[[1-(2-pyridinyl)cyclohexyl]methyl]-1h-indole-3-propanamide |
| SCHEMBL6249801 |
| 204066-82-0 |
| J-013285 |
| (s)-3-(1h-indol-3-yl)-2-methyl-2-(3-(4-nitrophenyl)ureido)-n-((1-(pyridin-2-yl)cyclohexyl)methyl)propanamide |
| Q27088274 |
| pd 168368 is known as an nmbr antagonist. |
| MS-30117 |
| HY-116216 |
| CS-0064383 |
| AKOS040759496 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " The first aim of this study was to pharmacologically compare the dose-response curves for scratching induced by intrathecally administered bombesin-related peptides versus morphine, which is known to elicit itch in humans." | ( Physiological function of gastrin-releasing peptide and neuromedin B receptors in regulating itch scratching behavior in the spinal cord of mice. Ko, MC; Sukhtankar, DD, 2013) | 0.39 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Neuromedin-B receptor | Homo sapiens (human) | Ki | 0.0002 | 0.0002 | 0.0008 | 0.0020 | AID42490 |
| Gastrin-releasing peptide receptor | Homo sapiens (human) | Ki | 0.0170 | 0.0002 | 0.0061 | 0.0170 | AID42630 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| bombesin receptor activity | Neuromedin-B receptor | Homo sapiens (human) |
| neuropeptide receptor activity | Neuromedin-B receptor | Homo sapiens (human) |
| neuropeptide receptor activity | Gastrin-releasing peptide receptor | Homo sapiens (human) |
| G protein-coupled peptide receptor activity | Gastrin-releasing peptide receptor | Homo sapiens (human) |
| neuropeptide binding | Gastrin-releasing peptide receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| cytosol | Neuromedin-B receptor | Homo sapiens (human) |
| plasma membrane | Neuromedin-B receptor | Homo sapiens (human) |
| plasma membrane | Neuromedin-B receptor | Homo sapiens (human) |
| plasma membrane | Gastrin-releasing peptide receptor | Homo sapiens (human) |
| plasma membrane | Gastrin-releasing peptide receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID42490 | Antagonism of recombinant human bombesin receptor (bb1) labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells | 1998 | Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18 | PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist. |
| AID42630 | In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin. | 1998 | Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18 | PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist. |
| AID1346439 | Human BB1 receptor (Bombesin receptors) | 2009 | Peptides, Aug, Volume: 30, Issue:8 | Characterization of putative GRP- and NMB-receptor antagonist's interaction with human receptors. |
| AID1346539 | Human BB2 receptor (Bombesin receptors) | 2009 | Peptides, Aug, Volume: 30, Issue:8 | Characterization of putative GRP- and NMB-receptor antagonist's interaction with human receptors. |
| AID1346497 | Rat BB1 receptor (Bombesin receptors) | 1999 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 290, Issue:3 | Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368. |
| AID1346539 | Human BB2 receptor (Bombesin receptors) | 1999 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 290, Issue:3 | Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (13.33) | 18.2507 |
| 2000's | 4 (26.67) | 29.6817 |
| 2010's | 9 (60.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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 weak demand-to-supply ratio for research on this compound.
| This Compound (12.01) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 15 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||