NAB-14 is a potent, selective negative allosteric modulator of GluN2C/2D-containing NMDA receptors with IC50 of 580 nM, >800-fold selective over GluN2A/GluN2 receptors; inhibits triheteromeric (GluN1/GluN2A/GluN2C) NMDARs with modestly reduced potency and efficacy compared to diheteromeric (GluN1/GluN2C/GluN2C) receptors; inhibits GluN2D-mediated synaptic currents in rat subthalamic neurons and mouse hippocampal interneurons, but has no effect on synaptic transmission in hippocampal pyramidal neurons.
(1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) is a Beta site APP Cleaving Enzymel (BACE1) inhibitor extracted from patent WO2012087237A1, compound 20a, has IC50s of 2.2 nM (TR-FRET assay) and 0.28 nM (sAPPp release assay), respectively[1].
COX-2-IN-23 (compound A10) is a potent both AChE and HDAC inhibitor with IC50 values of 0.12 and 0.23 nM. COX-2-IN-23 exhibits antioxidant activity and metal chelating properties. COX-2-IN-23 can be used in alzheimer's disease research[1].
Cyclodrine hydrochloride is a cholinergic (muscarinic, nicotinic) (mAChR and nAChR) receptor antagonist.
Ro 60-0175 is a potent, selective 5-HT2C receptor agonist with pKi of 9, 7.5, 5.4, 5.2 and 5.6 for human 5-HT2C, 2A, 1A, 6 and 7 receptors respectively; induces hypolocomotion in rats at doses greater than 0.5 mg/kg s.c.; (0.3 and 1 mg/kg s.c.) simultaneously reduces both unpunished and punished lever pressing, a profile consistent with sedation, induces sedative-like responses via 5-HT(2C) receptor activation in vivo.
Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect[1].
HBT1 is a novel potent AMPA receptor potentiator with lower agonistic effect compared with LY451395 and OXP1.
VU6028418 (VU 6028418) is a potent, highly selective, orally bioavailable M4 mAChR antagonist for the treatment of dystonia and other movement disorders.
Octamylamine is an anticholinergic and antispasmodic agent[1].
Levophacetoperane inhibits in vitro in a competitive manner, norepinephrin uptake and dopamine uptake.
Dinotefuran is an insecticide of the neonicotinoid class, its mechanism of action involves disruption of the insect's nervous system by inhibiting nicotinic acetylcholine receptors.Target: nAChR, Antiparasitic
(S)-(-)-HA 966 ((-)-HA 966), a γ-Hydroxybutyrate-like agent, is weakly active as an NMDA-receptor antagonist. (S)-(-)-HA 966 possesses muscle relaxant action and prevents enhanced mesocorticolimbic dopamine metabolism and behavioral correlates of restraint stress, conditioned fear[1][2].
Naltriben mesylate is a potent delta-2 receptor-selective antagonist, with Kis are 0.013, 19 and 152 nM for δ, μ and κ receptors respectively. Naltriben mesylate selectively attenuates alcohol intake in rats bred for alcohol preference[1][2].
MPX-004 is a potent GluN2A antagonist. MPX-004 inhibits GluN2A-containing NMDA receptors expressed in HEK cells with an IC50 of 79 nM. MPX-004 has no inhibitory effect on GluN2B or GluN2D receptor-mediated responses. MPX-004 has the potential for neuropsychiatric and developmental disorders research[1].
Rhodiosin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.420 μM and a Ki of 0.535 μM[1]. Rhodiosin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL[2]. Rhodiosin exhibits potent DPPH free radical scavenging activities, with an IC50 of 27.77 μM[3].
Solriamfetol hydrochloride (JZP-110 hydrochloride) is an orally active and selective dopamine and norepinephrine reuptake inhibitor with IC50s of 2.9 μM and 4.4 μM for dopamine and norepinephrine transporters, respectively. Solriamfetol hydrochloride has robust wake-promoting effects[1][2].
L-Glutamic acid-d5 is the deuterium labeled L-Glutamic acid. L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
Methylene blue (Basic Blue 9) hydrate is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue hydrate through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue hydrate is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue hydrate is a Tau aggregation inhibitor. Methylene blue hydrate reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation[1][2][3].
μ opioid receptor agonist 2 （Compound H-3）is an optically pure oxaspiro ring substituted pyrrolopyrazole derivative, acts as a MOR receptor agonist and can be used for the research of pain and pain related diseases[1].
Gepirone is a selectively and affinitive 5-HT1A agonist. Gepirone binds selectively to 5-HT1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research[1].
UFP-101 is a potent, selective, and competitive antagonist of the nociceptin/orphanin FQ (NOP) receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect[1][2].
MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively[1][2].
Vilazodone (EMD 68843; SB 659746A) is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist currently under clinical evaluation for the treatment of major depression.IC50 value:Target: SSRI; 5-HT1AVilazodone represents another option for the treatment of MDD. Vilazodone appears to have a favourable weight-gain profile based on short-term studies. Sexual side-effects were not consistently demonstrated when assessed using clinical rating scales but spontaneously reported AEs related to sexual functioning were observed. Additional controlled data regarding long-term efficacy and effectiveness will help characterise this new agent when used in maintenance treatment.
Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI).
Clomipramine D3 hydrochloride is a deuterium labeled Clomipramine hydrochloride. Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively[1][2].
Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
Etifoxine Hcl(HOE 36-801) is potentiator of GABAA receptor function in cultured neurons. Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors. IC50 value:Target: GABAA receptorEtifoxine exhibits anxiolytic activity in rodents and humans with no sedative, myorelaxant or mnesic side effects. Etifoxine acts as a ligand of the translocator protein (TSPO); promotes axonal regeneration.
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
(S)-Remoxipride ((-)-Remoxipride) is a selective dopamine D2-receptor antagonist with an IC50 value of 1.57 μM. (S)-Remoxipride can be used for the research of psychotic disorder[1].
Zimelidine dihydrochloride is a potent and selective inhibitor of serotonin 5-HT uptake and SERT. Zimelidine dihydrochloride is an antidepressant[1].