addiction

Fenobam shows inverse agonist activity which blocks the mGlu5 receptor basal activity(IC50: 84 nM). Fenobam has anxiolytic activity. Fenobam is a selective and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively).

Oxeladin citrate is a highly potent and effective cough suppressant, which can treat all types of cough of various etiologies. It is not related to opium or its derivatives, so treatment with oxeladin is no risk of addiction. And it has none of the side effects (such as hypnosis, respiratory depression, tolerance, constipation and analgesia) which are present when common antitussives. It can used at every age, as well as in patients with heart disease, since it is high level of safety and a great selectivity to act on the bulbar centre of cough.

Naltrexone hydrochloride (Naltrexone HCl) is a synthetic opioid antagonist used in the prevention of relapse of opiate addiction and alcoholism.

AZD-8529 mesylate is a highly selective, and orally bioavailable positive allosteric modulator of mGluR2 (EC50: 285 nM). It shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

BP 897 is a potent and selective agonist of dopamine D3 receptor and it is a weak dopamine D2 receptor antagonist, with Kis of 0.92 nM and 61 nM for D3 and D2 receptors. Which shows low affinities at D1 and D4 receptors (Kis, 3 and 0.3 μM, respectively).

OS-3-106 is a novel arylamide phenylpiperazines, as partial agonists at the D3R in the adenylyl cyclase inhibition assay.

BP 897 (2-Naphthalenecarboxamide, N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-) is a potent and selective dopamine D3 receptor agonist, and a weak dopamine D2 receptor antagonist, with Kis of 0.92 nM and 61 nM for D3 and D2 receptors, and shows low affinities at D1 and D4 receptors (Kis, 3 and 0.3 μM, respectively).

Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction. Pozanicline selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a no

Eglumetad (also known as LY354740) is an investigational compound developed by Eli Lilly and Company, currently under research for the treatment of anxiety disorders and substance addiction. This compound originates from glutamate, demonstrating a novel mechanism of action.

neuropeptide S receptor (NPSR) antagonist

NGB 2904 is a potent and selective antagonist of dopamine D3 receptor (Ki values are 1.4, 217, 223, 642, > 5000, > 10000 and > 10000 nM for D3, D2, 5-HT2, α1, D4, D1 and D5 receptors respectively). NGB2904 potently antagonizes mitogenesis stimulated by quinpirole (IC50 = 6.8 nM).

Potent TBK1 (TANK-binding kinase-1) inhibitor (IC50 = 6 nM). Inhibits the formation of autophagosomes in lung cancer cells. Newman et al (2012) TBK1 kinase addiction in lung cancer cells is mediated via autophagy of Tax1bp1/Ndp52 and non-canonical NF-κB signalling. PLoS ONE 7 e50672 PMID:23209807 |McIver et al (2012) Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKe kinases. Bioorg.Med.Chem.Lett. 22 7169 PMID:23099093

(S)-UFR2709 (hydrochloride) is a competitive nAChR antagonist with higher affinity for α4β2 nAChRs than for α7 nAChRs. It decreases anxiety and reduces ethanol consumption and preference in alcohol-preferring rats. As an anxiolytic agent, (S)-UFR2709 (hydrochloride) can be used for the study of nicotine addiction[1][2].

(S)-UFR2709 is a competitive antagonist of the nicotinic acetylcholine receptor (nAChR), showing greater affinity for α4β2 nAChRs over α7 nAChRs. It effectively reduces anxiety, ethanol consumption, and ethanol preference in alcohol-preferring rats, functions as an anxiolytic agent, and holds potential for investigating nicotine addiction.

Varenicline dihydrochloride is a Selective α4β2 nicotinic acetylcholine receptor partial agonist.

3-hydroxy-3-phenylpentanamide is a chiral compound belonging to the class of beta-hydroxyamides. In neurology, it has been shown to have neuroprotective effects against ischemic brain injury and cerebral hemorrhage. In psychiatry, it has been studied as a potential treatment for anxiety, depression and addiction. In oncology, it has been shown to have antitumor activity by inducing apoptosis and inhibiting tumor growth.

5-(2-aminoethyl)-4-methyl-1,3-thiazol-2-amine dihydrochloride is a potent and selective antagonist of metabotropic glutamate receptor 5 (mGluR5). It has been shown to be effective in several neurological disorders, including fragile X syndrome, autism spectrum disorders, and addiction.

CB1R Allosteric modulator 3 is a potent CB1R modulator that inhibits cAMP and β-Arrestin and can be used for the study of obesity and nicotine addiction.

RTI-7470-44 is a potent and selective human trace amine-associated receptor 1 (hTAAR1) antagonist (IC50: 8.4 nM) that crosses the blood-brain barrier. RTI-7470-44 increases the spontaneous firing rate of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain in mice. RTI-7470-44 can be used to study schizophrenia, drug addiction and Parkinson's disease (PD).

Neramexane Free Base is a drug related to memantine, which acts as an NMDA antagonist and has neuroprotective effects. It is being developed for various possible applications, including treatment of tinnitus, Alzheimer's disease, drug addiction and as an analgesic.

LCRF-0004 is a potent and selective RON receptor tyrosine kinase inhibitor. The RON receptor tyrosine kinase has been identified as an important mediator of KRAS oncogene addiction and is overexpressed in the majority of pancreatic cancers. Preclinical studies show that inhibition of RON function decreases pancreatic cancer cell migration, invasion, and survival and can sensitize pancreatic cancer cells to chemotherapy. RON receptor tyrosine kinase is a potential as a therapeutic target.

CTAP TFA, a potent and highly selective μ opioid receptor antagonist that effectively crosses the blood-brain barrier, exhibits a significant inhibition concentration (IC50) of 3.5 nM. It demonstrates extraordinary selectivity, being over 1200-fold more specific to μ opioid receptors than to δ opioid (IC50 = 4500 nM) and somatostatin receptors. This compound is primarily leveraged for researching L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction [1] [2].

Dynorphin (2-17), amide (porcine) is a dynorphin derivative from the opioid peptide class, synthesized from the precursor protein dynorphinogen, and exhibits analgesic properties, playing a pivotal role in regulating pain, addiction, and mood [1].

Orexin Receptor Modulator-1 is a compound utilized in the study of various conditions including substance addiction, panic disorder, anxiety, post-traumatic stress disorder (PTSD), pain, depression, seasonal affective disorder (SAD), eating disorders, and hypertension [1].