(4-Chlorophenyl)-(7-methyl-3-imidazo[1,2-a]pyridinyl)methanone, also known as **MK-0431** or **CP-99,994**, is a potent and selective **histamine H3 receptor antagonist**.
**What is a Histamine H3 Receptor Antagonist?**
* **Histamine** is a neurotransmitter that plays a role in various physiological processes, including sleep-wake cycles, appetite, and cognitive function.
* **Histamine H3 receptors** are found in the brain and other tissues, where they act as autoreceptors, meaning they regulate the release of histamine.
* **Antagonists** block the action of a receptor. In this case, a H3 antagonist prevents histamine from binding to the H3 receptor.
**Why is MK-0431 Important for Research?**
MK-0431 is a valuable research tool for several reasons:
1. **Understanding Histamine H3 Receptor Function:**
* MK-0431 allows researchers to study the role of histamine H3 receptors in various biological processes.
* By blocking the receptor, they can observe the effects of inhibiting histamine signaling.
2. **Development of New Drugs:**
* Histamine H3 antagonists have potential therapeutic applications in conditions like:
* **Cognitive disorders:** Improving memory, attention, and alertness.
* **Sleep disorders:** Promoting wakefulness and improving sleep quality.
* **Obesity:** Reducing appetite and promoting weight loss.
* MK-0431 serves as a lead compound for the development of new and improved drugs targeting the H3 receptor.
3. **Preclinical Studies:**
* MK-0431 has been used in preclinical animal studies to investigate the effects of H3 antagonism on:
* Learning and memory
* Sleep-wake cycles
* Appetite and food intake
* Anxiety and depression
**Important Note:** While MK-0431 shows promise as a potential drug, it is still in the early stages of research. It is not currently approved for medical use.
**In Summary:**
MK-0431 is a potent histamine H3 receptor antagonist that is valuable for research into the function of histamine H3 receptors and for the development of new drugs targeting this receptor.
| ID Source | ID |
|---|---|
| PubMed CID | 3776081 |
| CHEMBL ID | 1383128 |
| CHEBI ID | 114470 |
| Synonym |
|---|
| smr000126350 |
| (4-chlorophenyl)(7-methylimidazo[1,2-a]pyridin-3-yl)methanone |
| MLS000541492 |
| OPREA1_186700 |
| CHEBI:114470 |
| AKOS005103477 |
| (4-chlorophenyl)-(7-methylimidazo[1,2-a]pyridin-3-yl)methanone |
| HMS2342E10 , |
| 339103-69-4 |
| 3-(4-chlorobenzoyl)-7-methylimidazo[1,2-a]pyridine |
| 8K-420S , |
| CHEMBL1383128 |
| DTXSID80396276 |
| Q27195873 |
| (4-chlorophenyl)-(7-methyl-3-imidazo[1,2-a]pyridinyl)methanone |
| (4-chlorophenyl)(7-methylimidazo(1,2-a)pyridin-3-yl)methanone |
| mfcd00974160 |
| Class | Description |
|---|---|
| aromatic ketone | A ketone in which the carbonyl group is attached to an aromatic ring. |
| [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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 39.8107 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 2.1331 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
| BRCA1 | Homo sapiens (human) | Potency | 2.8184 | 0.8913 | 7.7225 | 25.1189 | AID624202 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 1.3971 | 0.0041 | 10.8903 | 31.5287 | AID504466; AID504467 |
| TDP1 protein | Homo sapiens (human) | Potency | 16.3601 | 0.0008 | 11.3822 | 44.6684 | AID686979 |
| P53 | Homo sapiens (human) | Potency | 11.2202 | 0.0731 | 9.6858 | 31.6228 | AID504706 |
| NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 3.5481 | 0.0126 | 2.4518 | 25.0177 | AID485313 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 16.3601 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
| parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 3.9811 | 3.5481 | 19.5427 | 44.6684 | AID743266 |
| ras-related protein Rab-9A | Homo sapiens (human) | Potency | 1.4125 | 0.0002 | 2.6215 | 31.4954 | AID485297 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 0.2818 | 0.0079 | 8.2332 | 1,122.0200 | AID2551 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 14.1254 | 1.9953 | 25.5327 | 50.1187 | AID624287 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| negative regulation of inflammatory response to antigenic stimulus | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| renal water homeostasis | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| G protein-coupled receptor signaling pathway | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| regulation of insulin secretion | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| cellular response to glucagon stimulus | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| G protein activity | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| adenylate cyclase activator activity | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| [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 | 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] | ||
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 (12.56) 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 | 5 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||