 | |
| Names | |
|---|---|
| IUPAC name 2-[3-[1-[(1R)-1,2-Dihydroacenaphthylen-1-yl]piperidin-4-yl]-2-oxobenzimidazol-1-yl]-N-methylacetamide | |
| Identifiers | |
| |
PubChem CID | |
CompTox Dashboard (EPA) | |
| Properties | |
| C27H28N4O2 | |
| Molar mass | 440.547 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
MT-7716 is an experimental opioid drug that could potentially be used in the treatment of alcohol addiction.
Unlike most opioids, MT-7716 does not appear to act through delta, kappa and mu opioid receptors, but instead is an agonist of the nociceptin receptor. [1]
A study has shown that MT-7716 was able to decrease alcohol self-administration and reduce alcohol withdrawal symptoms in rats. [2]
Another study was also able to show similar results, in addition to demonstrating MT-7716's ability to suppress stress-induced alcohol seeking. [3]
Dynorphins (Dyn) are a class of opioid peptides that arise from the precursor protein prodynorphin. When prodynorphin is cleaved during processing by proprotein convertase 2 (PC2), multiple active peptides are released: dynorphin A, dynorphin B, and α/β-neoendorphin. Depolarization of a neuron containing prodynorphin stimulates PC2 processing, which occurs within synaptic vesicles in the presynaptic terminal. Occasionally, prodynorphin is not fully processed, leading to the release of "big dynorphin". "Big dynorphin" is a 32-amino acid molecule consisting of both dynorphin A and dynorphin B.
An opioid antagonist, or opioid receptor antagonist, is a receptor antagonist that acts on one or more of the opioid receptors.
Quinpirole is a psychoactive drug and research chemical which acts as a selective D2 and D3 receptor agonist. It is used in scientific research. Quinpirole has been shown to increase locomotion and sniffing behavior in mice treated with it. At least one study has found that quinpirole induces compulsive behavior symptomatic of obsessive compulsive disorder in rats. Another study in rats show that quinpirole produces significant THC-like effects when metabolic degradation of anandamide is inhibited, supporting the hypothesis that these effects of quinpirole are mediated by cannabinoid CB1 receptors. Quinpirole may also reduce relapse in adolescent rat models of cocaine addiction.
Nociceptin/orphanin FQ (N/OFQ), a 17-amino acid neuropeptide, is the endogenous ligand for the nociceptin receptor. Nociceptin acts as a potent anti-analgesic, effectively counteracting the effect of pain-relievers; its activation is associated with brain functions such as pain sensation and fear learning.
The κ-opioid receptor or kappa opioid receptor, abbreviated KOR or KOP for its ligand ketazocine, is a G protein-coupled receptor that in humans is encoded by the OPRK1 gene. The KOR is coupled to the G protein Gi/G0 and is one of four related receptors that bind opioid-like compounds in the brain and are responsible for mediating the effects of these compounds. These effects include altering nociception, consciousness, motor control, and mood. Dysregulation of this receptor system has been implicated in alcohol and drug addiction.
The nociceptin opioid peptide receptor (NOP), also known as the nociceptin/orphanin FQ (N/OFQ) receptor or kappa-type 3 opioid receptor, is a protein that in humans is encoded by the OPRL1 gene. The nociceptin receptor is a member of the opioid subfamily of G protein-coupled receptors whose natural ligand is the 17 amino acid neuropeptide known as nociceptin (N/OFQ). This receptor is involved in the regulation of numerous brain activities, particularly instinctive and emotional behaviors. Antagonists targeting NOP are under investigation for their role as treatments for depression and Parkinson's disease, whereas NOP agonists have been shown to act as powerful, non-addictive painkillers in non-human primates.
Lobeline is a piperidine alkaloid found in a variety of plants, particularly those in the genus Lobelia, including Indian tobacco, Devil's tobacco, great lobelia, Lobelia chinensis, and Hippobroma longiflora. In its pure form, it is a white amorphous powder which is freely soluble in water.
SB-277,011A is a drug which acts as a potent and selective dopamine D3 receptor antagonist, which is around 80–100 times selective for D3 over D2, and lacks any partial agonist activity.
JTC-801 is an opioid analgesic drug used in scientific research.
PPAR agonists are drugs which act upon the peroxisome proliferator-activated receptor. They are used for the treatment of symptoms of the metabolic syndrome, mainly for lowering triglycerides and blood sugar.
Ro64-6198 is an opioid drug used in scientific research. It acts as a potent and selective agonist for the nociceptin receptor, also known as the ORL-1 receptor, with over 100x selectivity over the other opioid receptors. It produces anxiolytic effects in animal studies equivalent to those of benzodiazepine drugs, but has no anticonvulsant effects and does not produce any overt effects on behaviour. However it does impair short-term memory, and counteracts stress-induced anorexia. It also has antitussive effects, and reduces the rewarding and analgesic effects of morphine, although it did not prevent the development of dependence. It has been shown to reduce alcohol self-administration in animals and suppressed relapses in animal models of alcoholism, and ORL-1 agonists may have application in the treatment of alcoholism.
3-( ethynyl)pyridine (MTEP) is a research drug that was developed by Merck & Co. as a selective allosteric antagonist of the metabotropic glutamate receptor subtype mGluR5. Identified through structure-activity relationship studies on an older mGluR5 antagonist MPEP, MTEP has subsequently itself acted as a lead compound for newer and even more improved drugs.
JDTic is a selective, long-acting ("inactivating") antagonist of the κ-opioid receptor (KOR). JDTic is a 4-phenylpiperidine derivative, distantly related structurally to analgesics such as pethidine and ketobemidone, and more closely to the MOR antagonist alvimopan. In addition, it is structurally distinct from other KOR antagonists such as norbinaltorphimine. JDTic has been used to create crystal structures of KOR [ PDB: 4DJH, 6VI4].
SKF-97,541 is a compound used in scientific research which acts primarily as a selective GABAB receptor agonist. It has sedative effects in animal studies and is widely used in research into potential treatment of various types of drug addiction.
SoRI-9409 is a mixed mu opioid receptor partial agonist and delta opioid receptor antagonist, used in biomedical research. It produces moderate analgesic effects without development of tolerance and with reduced withdrawal symptoms compared to standard opioid analgesics, as well as showing anti-addictive effects that may be useful in the treatment of alcoholism.
The central nucleus of the amygdala is a nucleus within the amygdala. It "serves as the major output nucleus of the amygdala and participates in receiving and processing pain information."
LY-255582 is a phenylpiperidine non-selective opioid antagonist. It has been shown to reduce ethanol consumption in experiments carried out on rats. It has also been shown to reduce food and water consumption in rats.
Marisa Roberto is an Italian-American neuroscientist and professor in the Department of Molecular Medicine and Neuroscience at The Scripps Research Institute in La Jolla, California. Roberto is recognized for her contributions to the understanding of alcohol addiction, specifically for her research on the effects of alcohol and neuromodulators on synaptic transmission in the central amygdala, a critical addiction-related brain region.
Ro65-6570 is an opioid drug. It has a potential use in preventing the addiction to other opioids.
SCH-221510 is an experimental opioid drug. It has potential as an analgesic and as a treatment to addiction of certain drugs.
