(9-chloro-5,6,7,8-tetrahydroacridin-3-yl)-(4-methyl-1-piperidinyl)methanone, often referred to by its simpler name **THA**, is a **synthetic compound** that has gained significant attention in the field of **neuroscience**. It's not a naturally occurring substance but has been synthesized specifically for research purposes.
Here's what makes THA important:
* **Highly Selective Ligand for Nicotinic Acetylcholine Receptors:** THA is a potent and selective ligand for a specific subtype of nicotinic acetylcholine receptors (nAChRs) known as **α4β2 nAChRs**. These receptors are found throughout the central nervous system and play a crucial role in regulating various brain functions including learning, memory, attention, and reward.
* **Potential Therapeutic Applications:** The selectivity of THA for α4β2 nAChRs has sparked interest in its potential therapeutic use for conditions like:
* **Alzheimer's disease:** α4β2 nAChRs are implicated in cognitive decline associated with Alzheimer's, and THA might be able to improve cognitive function.
* **Schizophrenia:** Research suggests that dysregulation of α4β2 nAChRs could be involved in schizophrenia, and THA might have potential as an antipsychotic agent.
* **Addiction:** THA has shown promise in preclinical studies as a potential treatment for nicotine addiction.
* **Research Tool:** Beyond its therapeutic potential, THA is a valuable tool for researchers studying the role of α4β2 nAChRs in the brain. It allows scientists to investigate these receptors in more detail, leading to a better understanding of their function and how they might be targeted therapeutically.
**Important Note:** It's crucial to emphasize that THA is still in the research phase. While it shows promise, its safety and efficacy in humans haven't been fully established. More research is needed before it can be considered for clinical use.
**Summary:** THA is a synthetic compound with selective affinity for α4β2 nAChRs. This selectivity makes it a promising candidate for treating neurological and psychiatric disorders and a valuable tool for research on these receptors.
ID Source | ID |
---|---|
PubMed CID | 6622379 |
CHEMBL ID | 1472496 |
CHEBI ID | 105040 |
Synonym |
---|
HMS2613I17 |
CHEMDIV3_009937 , |
9-chloro-6-[(4-methylpiperidin-1-yl)carbonyl]-1,2,3,4-tetrahydroacridine |
MLS000731298 , |
smr000309573 |
IDI1_027847 |
CHEBI:105040 |
BRD-K89438694-001-01-0 |
9-chloro-6-(4-methylpiperidine-1-carbonyl)-1,2,3,4-tetrahydroacridine |
AKOS001825887 |
HMS1501D15 |
(9-chloro-5,6,7,8-tetrahydroacridin-3-yl)-(4-methylpiperidin-1-yl)methanone |
CHEMBL1472496 |
(9-chloro-5,6,7,8-tetrahydroacridin-3-yl)-(4-methylpiperidino)methanone |
cid_6622379 |
bdbm48850 |
(9-chloranyl-5,6,7,8-tetrahydroacridin-3-yl)-(4-methylpiperidin-1-yl)methanone |
(9-chloro-5,6,7,8-tetrahydroacridin-3-yl)-(4-methyl-1-piperidinyl)methanone |
HMS3441B12 |
Q27182718 |
Class | Description |
---|---|
acridines | |
[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, Beta-lactamase | Escherichia coli K-12 | Potency | 31.6228 | 0.0447 | 17.8581 | 100.0000 | AID485341 |
Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 22.3872 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 19.0115 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
TDP1 protein | Homo sapiens (human) | Potency | 23.1093 | 0.0008 | 11.3822 | 44.6684 | AID686978 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 4.4668 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
huntingtin isoform 2 | Homo sapiens (human) | Potency | 11.2202 | 0.0006 | 18.4198 | 1,122.0200 | AID1688 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 12.5893 | 0.0079 | 8.2332 | 1,122.0200 | AID2546 |
Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 1.0000 | 1.9953 | 25.5327 | 50.1187 | AID624287 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
fatty acid synthase | Homo sapiens (human) | IC50 (µMol) | 6.0700 | 0.1660 | 5.6472 | 18.2000 | AID624326; AID624327 |
eukaryotic translation initiation factor 4 gamma 1 isoform 4 | Homo sapiens (human) | IC50 (µMol) | 50.0000 | 1.1500 | 12.6200 | 25.6529 | AID855 |
eukaryotic translation initiation factor 4E isoform 1 | Mus musculus (house mouse) | IC50 (µMol) | 50.0000 | 1.1500 | 12.6200 | 25.6529 | AID855 |
[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 |
---|---|---|---|---|
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. |
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. |
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. |
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
[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 (14.29) | 29.6817 |
2010's | 5 (71.43) | 24.3611 |
2020's | 1 (14.29) | 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 (12.20) 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 | 7 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |