CGP 54626 (hydrochloride) is a selective antagonist of GABAB receptor with an IC50 value of 4 nM. CGP 54626 (hydrochloride) can be used to investigate the role of GABAB receptors in neurological signaling[1].
Oxotremorine M iodide is a potent and selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms[1].
Atropine sulfate monohydrate is a competitive muscarinic acetylcholine receptor antagonist.Target: mAChRAtropine is a naturally occurring tropane alkaloid extracted from deadly nightshade (Atropa belladonna), Jimson weed (Datura stramonium), mandrake (Mandragora officinarum) and other plants of the family Solanaceae. Atropine is a competitive antagonist of the muscarinic acetylcholine receptors (acetylcholine being the main neurotransmitter used by the parasympathetic nervous system). Atropine dilates the pupils, increases heart rate, and reduces salivation and other secretions [1].
Tavapadon (PF 6649751, PF-06649751) is an orally available dopamine D1 receptor partial agonist for treatment of Parkinson's disease. Parkinson Disease Discontinued
Hexafluorenium dibromide (Mylaxen) is a potent cholinesterase (ChE) inhibitor with pI50 value of 6.96 and Ki value of 2.4 nM for human plasma cholinesterase (ChE)[1].
Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
AMPA receptor modulator-6 is an AMPA receptor positive allosteric modulator (PAM). AMPA receptor modulator-6 can be used in the study of neurological diseases[1].
Pancopride is a new potent and selective 5-HT3 receptor antagonist.
NMDA-IN-2 (compound 6b), a Procaine derivative, is a NMDA receptor 2B subtype inhibitor[1].
Eptinezumab is a human monoclonal antibody. Eptinezumab binds to calcitonin gene-related peptide (CGRP) and blocks its binding to the receptor. Eptinezumab can be used for the prevention of migraine in adults[1].
Agomelatine (L(+)-Tartaric acid) is a antidepressant, which is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor. Target: 5-HT 2c receptor Agomelatine L(+)-Tartaric acid is an antidepressant drug. It is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor. Activation of 5-HT2C receptors by serotonin inhibits dopamine and norepinephrine release. Antagonism of 5-HT2C results in an enhancement of DA and NE release and activity of frontocortical dopaminergic and adrenergic pathways [1]. A total of 42 rats were divided into 7 groups as each composed of 6 rats: (1) intact, (2) 40 mg/kg agomelatine, (3) 140 mg/kg N-acetylcysteine (NAC), (4) 2 g/kg paracetamol, (5) 2 g/kg paracetamol + 140 mg/kg NAC, (6) 2 g/kg paracetamol + 20 mg/kgagomelatine, and (7) 2 g/kg paracetamol + 40 mg/kg agomelatine groups. Paracetamol-induced hepatotoxicity was applied and liver and blood samples were analyzed histopathologically and biochemically. There were statistically significant increases in the activities of aspartate aminotransferase, alanine aminotransferase, levels of tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) and 8-iso-prostane, and decreases in the activity of superoxide dismutase and level of glutathione in the group treated with paracetamol. Administration of agomelatine and NAC separately reversed these changes significantly [2].Clinical indications: Depression; Obsessive compulsive disorderFDA Approved Date: October 2011Toxicity: Hyperhidrosis; Abdominal pain; Nausea; Vomiting; Diarrhoea; Constipation; Back pain; Fatigue
SDZ 220-581 is a potent, competitive antagonist at the NMDA glutamate receptor subtype(pKi= 7.7).IC50 Value: Target: NMDA receptorin vitro: Wake-promoting doses of LSN2463359 and LSN2814617 attenuated deficits in performance induced by the competitiveNMDA receptor antagonist SDZ 220,581 in two tests of operant behaviour: the variable interval 30 s task and the DMTP task [1].in vivo: Administration of SDZ 220-581 or CGS 19755 was associated with a robust reduction in PPI, whereas L-701,324, 4-Cl-KYN or MLA failed to alter PPI [2]. With the most active agent, SDZ 220-581, full protection against maximal electroshock seizures (MES) was obtained at oral doses of 10 mg/kg in rats and in mice. The compound had a fast onset (< or = 1 hr) and a long duration (> or = 24 hr) of action [3]. Rats were pretreated with clozapine (0 or 5.0 mg/kg) or haloperidol (0 or 0.1 mg/kg), together with SDZ 220-581 (0 or 2.5 mg/kg), and tested. SDZ 220-581 and SDZ EAB-515 decreased PPI without affecting startle magnitude [4].
Otaplimastat (SP-8203), a matrix metalloproteinase (MMP) inhibitor, blocks N-methyl-D-aspartate (NMDA) receptor-mediated excitotoxicity in a competitive manner. Otaplimastat also exhibits anti-oxidant activity. Otaplimastat can be used for the research of brain ischemic injury[1][2][3].
SB-737050A is a potent 5-HT6 antagonist to prevent relapse into addiction[1].
Acacetin-7-O-β-D-galactopyranoside is a flavonoid that can be isolated from flower heads of Chrysanthemum morifolium. Acacetin-7-O-β-D-galactopyranoside inhibits AChE activity and can be used for research of Alzheimer’s disease[1].
Indazole, also called isoindazole, a heterocyclic aromatic organic compound. Its derivatives display a broad variety of biological activities including anti-inflammatory, antibacterial, anti-HIV, antiarrhythmic, antifungal and antitumour properties. Indazole and its derivatives can be used for research of cancer, neurological disorders, cardiovascular diseases, gastrointestinal diseases[1][2][3][4][5].
α-Conotoxin MII (α-CTxMII), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII (α-CTxMII) potently blocks β3-containing neuronal nicotinic receptors [1][2][3].
mGAT-IN-1 (compound 28) is a potent and non-selective GAT inhibitor. mGAT-IN-1 has a high inhibitory potency toward mGAT3, with an IC50 of 2.5 μM and pIC50 of 5.61[1].
2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B (GABAB) receptor antagonist. 2-Hydroxysaclofen can abolish nicotine-induced hypolocomotor effects and increases the antinociceptive effects. 2-Hydroxysaclofen can stimulate luteinizing hormone (LH) secretion in female rats[1][2][3].
NLX-204 (NLX204) is a potent, selective, ERK1/2 phosphorylation-preferring serotonin 5 HT1A receptor agonist with pEC50 of 9.37; shows promising pharmacokinetic profile, also robustly stimulates ERK1/2 phosphorylation in rat cortex and showed highly potent (MED=0.16 mg/kg) and efficacious antidepressant-like activity, totally eliminating immobility in the rat Porsolt test.
Trihexyphenidyl hydrochloride is an antiparkinsonian agent of the antimuscarinic class, binds to the M1 muscarinic receptor.
Quinelorane dihydrochloride (LY163502) is a potent dopamine D3/D2 receptor agonist. Quinelorane has the potential for neurological and psychiatric disorders research[1][2].
α-Methylserotonin is a potent and selective agonist of 5-HT2 receptor.α-Methylserotonin is an analogue of serotonin formed in vivo from α-methyltryptophan.α-Methylserotonin mediates the lymphatic smooth muscle contraction and prevents the up-regulation of serotonin-receptor-mediated phosphoinositide hydrolysis[1][2][3].
Molindone is a therapeutic antipsychotic, used in the treatment of schizophrenia, works by blocking the effects of dopamine in the brain, leading to diminished psychoses.
Eucalyptol-d6 is deuterium labeled Eucalyptol. Eucalyptol is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β.
Y1 receptor antagonist 1, an isomer of H-409/22, is a neuropeptide Y1 receptor antagonist.