addiction

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).

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.

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).

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).

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).

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.

7-Keto DHEA binds to the gamma-aminobutyric acid (GABA) receptor. Studies 7-Keto DHEA reduces ethanol intake in rat models, indicating a modulatory effect on alcohol consumption behavior. 7-Keto DHEA therefore exhibits potential as a investigational compound of alcohol dependence disorders, contributing to the broader field of addiction research.

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.

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

GSK1521498 free base is an effective and selective μ-opioid receptor antagonist with potential applications in obesity, alcoholism, and drug addiction.

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.

VU0469650 hydrochloride is a brain-penetrant negative allosteric modulator of the metabotropic glutamate receptor 1 (mGluR1). It inhibits glutamate-induced calcium flux in cells expressing human mGluR1 with an IC50 of 99 nM. VU0469650 hydrochloride holds potential for research into central nervous system disorders such as anxiety, addiction, and epilepsy.

Anticanceragent 192 (compound XXI) is a steroid-based histamine H3 receptor antagonist with no affinity for muscarinic and hERG receptors. It shows considerable stability in human and rat liver microsomes. Additionally, in addiction tests conducted on rats, Anticanceragent 192 enhances cognitive levels and reduces addiction severity.

ML 190 is a potent and selective κ opioid receptor (KOR) antagonist (Ki=129 nM), exhibiting an IC50=150 nM in β-arrestin assays, suitable for studying drug addiction.

YQA14 is a selective, high-affinity dopamine D3 receptor antagonist that inhibits cocaine self-administration in rats and mice, applicable for opioid addiction research.

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.