Page last updated: 2024-11-13
orexin-a
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 56842143 |
| MeSH ID | M0287275 |
Synonyms (10)
| Synonym |
|---|
| 205599-75-3 |
| orexin a |
| orexin-a |
| orexine a |
| unii-8rdy08v4vc |
| 8rdy08v4vc , |
| oroxin-a |
| HB2937 |
| xplpdccrqktcscrlyellhgagnhaagiltl (modifications: c-terminal amide; x-1 = glp; disulfide bonds: 6-12, 7-14) |
| c152h243n47o44s4 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (3)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Orexin receptor type 1 | Homo sapiens (human) | Ki | 0.0129 | 0.0003 | 0.2876 | 3.1623 | AID150548 |
| [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) |
|---|---|---|---|---|---|---|---|
| Orexin receptor type 1 | Homo sapiens (human) | EC50 (µMol) | 0.0101 | 0.0001 | 0.5062 | 2.5000 | AID1062207; AID1878169; AID767535 |
| Orexin receptor type 2 | Homo sapiens (human) | EC50 (µMol) | 0.0131 | 0.0001 | 0.0199 | 0.0600 | AID1062205; AID1878172; AID767534 |
| Cytochrome P450 1A2 | Homo sapiens (human) | EC50 (µMol) | 0.0011 | 0.0003 | 0.2069 | 2.0000 | AID1062205 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (34)
Molecular Functions (19)
Ceullar Components (4)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Orexin receptor type 1 | Homo sapiens (human) |
| synapse | Orexin receptor type 1 | Homo sapiens (human) |
| plasma membrane | Orexin receptor type 1 | Homo sapiens (human) |
| plasma membrane | Orexin receptor type 2 | Homo sapiens (human) |
| synapse | Orexin receptor type 2 | Homo sapiens (human) |
| plasma membrane | Orexin receptor type 2 | Homo sapiens (human) |
| endoplasmic reticulum membrane | Cytochrome P450 1A2 | Homo sapiens (human) |
| intracellular membrane-bounded organelle | Cytochrome P450 1A2 | Homo sapiens (human) |
| intracellular membrane-bounded organelle | Cytochrome P450 1A2 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Bioassays (11)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID51935 | Functional potency was determined by concentration required for activation of OX1 (Orexin-1) receptor expressed in chinese hamster ovary cells (CHO) and increasing the intracellular calcium concentration | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5 | Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor. |
| AID767534 | Agonist activity at OX2 receptor (unknown origin) expressed in RD-HGA16 cells assessed as calcium mobilization by fluorescence assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor. |
| AID1062205 | Agonist activity at human OX2 receptor overexpressed in CHO-RD-HGA16 cells assessed as calcium mobilization after 15 mins by fluorescence assay | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12 | Truncated Orexin Peptides: Structure-Activity Relationship Studies. |
| AID1062207 | Agonist activity at human OX1 receptor overexpressed in CHO-RD-HGA16 cells assessed as calcium mobilization after 15 mins by fluorescence assay | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12 | Truncated Orexin Peptides: Structure-Activity Relationship Studies. |
| AID767535 | Agonist activity at OX1 receptor (unknown origin) expressed in RD-HGA16 cells assessed as calcium mobilization by fluorescence assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor. |
| AID1062203 | Selectivity ratio of EC50 for human OX2 receptor to EC50 for human OX1 receptor | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12 | Truncated Orexin Peptides: Structure-Activity Relationship Studies. |
| AID1878175 | Selectivity index, ratio of EC50 for agonist activity at OX1R (unknown origin) to EC50 for agonist activity at OX2R (unknown origin) | |||
| AID1878169 | Agonist activity at OX1R (unknown origin) | |||
| AID150548 | Binding affinity to Orexin receptor type 1 was determined using laser scanning cytometry | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5 | Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor. |
| AID1249695 | Induction of wakefullness in C57BL/6J mouse assessed as increase in wake time by measuring EEG/EMG signals at 3 nmol, icv dosed on every other day during light phase | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20 | Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists. |
| AID1878172 | Agonist activity at OX2R (unknown origin) | |||
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (5)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (20.00) | 29.6817 |
| 2010's | 3 (60.00) | 24.3611 |
| 2020's | 1 (20.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 57.96
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 very strong demand-to-supply ratio for research on this compound.
| This Compound (57.96) All Compounds (24.57) |
Study Types
| 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 | 5 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||