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| PubChem CID | |
| Chemical and physical data | |
| Formula | C13H11FIN3 |
| Molar mass | 355.155 g·mol−1 |
| 3D model (JSmol) | |
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AGH-192 is a potent and selective, water soluble, orally bioavailable and brain penetrant full agonist at the 5HT7 serotonin receptor, derived from the older drug AGH-107. In animal tests it showed activity indicative of potential application in the treatment of neuropathic pain. [1]
The oxytocin receptor, also known as OXTR, is a protein which functions as receptor for the hormone and neurotransmitter oxytocin. In humans, the oxytocin receptor is encoded by the OXTR gene which has been localized to human chromosome 3p25.
Transient receptor potential cation channel subfamily V member 4 is an ion channel protein that in humans is encoded by the TRPV4 gene.
Transient receptor potential cation channel subfamily M (melastatin) member 8 (TRPM8), also known as the cold and menthol receptor 1 (CMR1), is a protein that in humans is encoded by the TRPM8 gene. The TRPM8 channel is the primary molecular transducer of cold somatosensation in humans. In addition, mints can desensitize a region through the activation of TRPM8 receptors.
The 5-HT7 receptor is a member of the GPCR superfamily of cell surface receptors and is activated by the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) The 5-HT7 receptor is coupled to Gs (stimulates the production of the intracellular signaling molecule cAMP) and is expressed in a variety of human tissues, particularly in the brain, the gastrointestinal tract, and in various blood vessels. This receptor has been a drug development target for the treatment of several clinical disorders. The 5-HT7 receptor is encoded by the HTR7 gene, which in humans is transcribed into 3 different splice variants.
The beta-3 adrenergic receptor (β3-adrenoceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the human gene encoding it.
Eglumetad is a research drug developed by Eli Lilly and Company, which is being investigated for its potential in the treatment of anxiety and drug addiction. It is a glutamate derived compound and its mode of action implies a novel mechanism.
5-Carboxamidotryptamine (5-CT) is a tryptamine derivative closely related to the neurotransmitter serotonin.
SB-699551 is a drug which was the first compound developed to act as a selective antagonist for the serotonin receptor 5-HT5A, with selectivity of around 100x over other serotonin receptor subtypes. Multiple therapeutic roles have been suggested for 5-HT5A ligands due to the presence of this receptor in several areas of the brain, but research is still at an early stage, In animal studies, SB-699551 was found to block cue-mediated responding to LSD, again suggesting an antipsychotic type of activity. It also reduces the viability of certain types of cancer cells in vitro, suggesting the 5-HT5A receptor as a possible target for novel chemotherapy drugs.
ABT-724 is a drug which acts as a dopamine agonist, and is selective for the D4 subtype. It was developed as a possible drug for the treatment of erectile dysfunction, although poor oral bioavailability means alternative drugs such as ABT-670 may be more likely to be developed commercially. Nonetheless, it continues to be used in scientific research into the function of the D4 receptor.
PHA-543,613 is a drug that acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatment for cognitive deficits in schizophrenia. It reduces excitotoxicity and protects striatal dopaminergic neurons in rat models. It also potentiates cognitive enhancement from memantine, decreases dynorphin release and inhibits GSK-B3.
Tedalinab (GRC-10693) is a drug developed by Glenmark Pharmaceuticals for the treatment of osteoarthritis and neuropathic pain, which acts as a potent and selective cannabinoid CB2 receptor agonist. It has a very high selectivity of 4700x for CB2 over the related CB1 receptor, has good oral bioavailability and has shown promising safety results and effective analgesic and antiinflammatory actions in early clinical trials. Many related compounds are known, most of which also show high CB2 selectivity.
LBP-1 is a drug originally developed by Organon for the treatment of neuropathic pain, It acts as a potent and selective cannabinoid receptor agonist, with high potency at both the CB1 and CB2 receptors, but low penetration of the blood–brain barrier. This makes LBP-1 peripherally selective, and while it was effective in animal models of neuropathic pain and allodynia, it did not produce cannabinoid-appropriate responding suggestive of central effects, at any dose tested.
The sphingosine-1-phosphate receptors are a class of G protein-coupled receptors that are targets of the lipid signalling molecule Sphingosine-1-phosphate (S1P). They are divided into five subtypes: S1PR1, S1PR2, S1PR3, S1PR4 and S1PR5.
PSB-CB5 (CID-85469571) is a compound which acts as an antagonist at the former orphan receptor GPR18, and is the first selective antagonist characterised for this receptor, with an IC50 of 279nM, and good selectivity over related receptors (over 36x selectivity vs CB1 and GPR55, and 14x vs CB2.) As all previously known antagonists for GPR18 also antagonise GPR55, it has been difficult to separate the effects of these two receptor targets, so the discovery of a selective GPR18 antagonist is expected to be useful in research into the actions of this receptor.
A-971432 is an orally bioavailable selective agonist of sphingosine-1-phosphate receptor 5 (S1PR5) discovered at AbbVie. It was discovered using high-throughput chemistry. S1P5 agonists have been proposed as an innovative mechanism for the treatment of neurodegenerative disorders such as Alzheimer's disease and lysosomal storage disorders such as Niemann–Pick disease. Stimulation of S1PR5 with A-971432 has been shown to preserve blood-brain barrier integrity and exert a therapeutic effect in an animal model of Huntington’s disease.
R7 is a small-molecule flavonoid and orally active, potent, and selective agonist of the tropomyosin receptor kinase B (TrkB) – the main signaling receptor for the neurotrophin brain-derived neurotrophic factor (BDNF) – which is under development for the treatment of Alzheimer's disease. It is a structural modification and prodrug of tropoflavin (7,8-DHF) with improved potency and pharmacokinetics, namely oral bioavailability and duration.
AGH-107 is a potent, selective, water-soluble and brain penetrant full agonist at the 5HT7 serotonin receptor. AGH-107 is one of the few examples of low-basicity aminergic receptor agonists, which may underlie its high selectivity over the related central nervous system targets. AGH-107 was found to reverse the impairment in novel object recognition caused by MK-801 in mice. The relatively short half-life in rodents inhibited its use as a molecular probe.
AH-494 is a potent and selective, water-soluble full agonist at the 5HT7 serotonin receptor. It is a close derivative of the known chemical probe 5-Carboxamidotryptamine, as well as of the more lipophilic indole-imidazoles: AGH-107 and AGH-192. It has been shown to exhibit favorable ADMET profile in in vitro assays.
C286, is a potent, orally bioavailable retinoic acid receptor beta (RARβ) agonist with good selectivity over the RARα, and RARγ receptors. This molecule increases neurite outgrowth in vitro and stimulates sensory axon regrowth in vivo in a rodent model of crush and avulsion injury, and is being evaluated for the treatment of nerve injury.