AChE/BuChE-IN-4(compound 4a) is aorally activeandbrain-penetrantmultitarget-directedAChE/BuChEinhibitor againstAChEandBuChE, with theIC50of 2.08 and 7.41 μM[1].
SB 204741 is a selective and high affinity 5-HT2B antagonist with a pKi value of 7.1[1].
W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 µM, respectively[1][2]. W-7 hydrochloride induces apoptosis and has antitumor activity[3].
Carpro-AM1 is a dual-acting FAAH/substrate-selective COX inhibitor with an IC50 value of 94 nM for FAAH[1].
S16961 is a nicotinic receptor agonist.
4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine is a potent amyloid imaging agent which binds to Amyloid-β (1-40) with a KD of 1.7 nM.
CP-465022 is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes[1][2].
Vilazodone Hydrochloride is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
AF-DX 384 is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively)[1]. AF-DX 384 reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine[2].
Temiverine hydrochloride is a synthesized drug that is expected to have anticholinergic action.
Setiptiline is a serotonin receptor antagonist.IC50 value:Target: 5-HT receptorSetiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine. From Wikipedia.
Rimacalib is a Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC50s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.
SB-205384 is a GABAA receptor modulator. The primary effect of SB-205384 on GABAA-activated currents is a prolonged response decay half-life upon removal of the agonist[1].
Myosmine, a specific tobacco alkaloid in nuts and nut products, has low affinity for a4b2 nicotinic acetylcholinergic receptors (nAChR) with a Ki of 3300 nM[1][2].
FAAH-IN-2 is a potent FAAH(fatty acid amide hydrolase) inhibitor extracted from Patent WO/2008/100977A2.
Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer's disease[1].
Isorosmanol is an abietane-type diterpene isolated from the leaves of sage, with antioxidant, neuroprotective and neurotrophic effects. Isorosmanol inhibits AChE activity and melanin synthesis[1][2][3].
7β-Hydroxybufalin is a bufadienolide that isolated from the venom of Bufo bufo gargarizans. 7β-Hydroxybufalin inhibits α-glucosidase and acetylcholinesterase[1].
Tulrampator (CX-1632) is an orally bioavailable positive allosteric modulator of AMPA receptor (AMPAR)[1]. Antidepressant[1].
NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC50s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively[1]. NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion[2].
(R)-VU 6008667, an active enantiomer of VU6008667, is a orally active acetylcholine receptor subtype 5 (M5 NAM) inhibitor with IC50 values of 1.2 μM (human) and 1.6 μM (rat), respectively. (R)-VU6008667 is selective for M5 over M1-4, high CNS penetration[1].
5,7-Dimethoxyluteolin, a 5,7-dimethylluteolin derivative, is a dopamine transporter (DAT) activator with an EC50 of 3.417 μM[1].
SAGE-217 is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
Imperatorin is an effective of NO synthesis inhibitor (IC50=9.2 μmol), which also is a BChE inhibitor (IC50=31.4 μmol). Imperatorin is a weak agonist of TRPV1 with EC50 of 12.6±3.2 μM.
Solifenacin is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
Venlafaxine is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class.Target: SNRIVenlafaxine is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class. First introduced by Wyeth in 1993, now marketed by Pfizer, it is licensed for the treatment of major depressive disorder (MDD), as a treatment for generalized anxiety disorder, and comorbid indications in certain anxiety disorders with depression. In 2007, venlafaxine was the sixth most commonly prescribed antidepressant on the U.S. retail market, with 17.2 million prescriptions.Venlafaxine is a bicyclic antidepressant, and usually categorized as a serotonin-norepinephrine reuptake inhibitor (SNRI), but it has been referred to as a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI). It works by blocking the transporter "reuptake" proteins for key neurotransmitters affecting mood, thereby leaving more active neurotransmitters in the synapse. The neurotransmitters affected are serotonin and norepinephrine. Additionally, in high doses it weakly inhibits the reuptake of dopamine, with recent evidence showing that the norepinephrine transporter also transports some dopamine as well, since dopamine is inactivated by norepinephrine reuptake in the frontal cortex. The frontal cortex largely lacks dopamine transporters; therefore, venlafaxine can increase dopamine neurotransmission in this part of the brain. Venlafaxine interacts with opioid receptors (mu-, kappa1- kappa3- and delta-opioid receptor subtypes) as well as the alpha2-adrenergic receptor, and was shown to increase pain threshold in mice. When mice were tested with a hotplate analgesia meter (to measure pain), both venlafaxine and mirtazapine induced a dose-dependent, naloxone-reversible antinociceptive effect following intraperitoneal injection. These findings suggest venlafaxine's seemingly superior efficacy in severe depression as narcotics become increasingly used as a measure of last resort for refractory cases.
Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system[1].
Cassiaside B2 is a protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A) inhibitor. Cassiaside B2 possesses antiallergic and is a 5-HT2C receptor agonist[1][2].[3]..
PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 7.3 nM in BACE1 binding assay.
Sultopride-d5 (LIN-1418-d5) is the deuterium labeled Sultopride. Sultopride (LIN-1418) is a selective antagonist of dopamine D2 receptor[1][2].