GNE 0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively.
α-Conotoxin BuIA is a paralytic peptide neurotoxin and a competitive nAChR antagonist, with IC50s of 0.258 nM (α6/α3β2), 1.54 nM (α6/α3β4), 5.72 nM (α3β2), respectively. α-Conotoxin BuIA can be used to distinguish nAChRs containing β2- and β4-subunit, respectively. α-Conotoxin BuIA distinguishes among αxβ2 nAChRs with a rank order potency of α6>α3>α2>α4[1].
Methiothepin maleate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
Bifemelane hydrochloride is a potent, selective and competitive inhibitor of monoamine oxidase A (MAO-A), with a Ki of 4.20 μM, and it also inhibits MAO-B noncompetitively with a Ki of 46.0 μM. Bifemelane hydrochloride has a potent antidepressant activity and can be used for the research of cognitive and emotional disturbances related to cerebrovascular disease[1][2].
BuChE-IN-6 (compound 1b) is a potent and selective BuChE (butyrylcholinesterase) inhibitor, with IC50 values of 0.46 and 0.51 μM for eqBuChE and hBuChE, respectively. BuChE-IN-6 also inhibits Aβ42 self-aggregation[1].
L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors affinity. L-745870 hydrochloride has excellent brain penetration[1][2][3].
Cyclo(glycyl-L-leucyl) (Cyclo(leu-gly)), a neuropeptide, down-regulates dopamine (DA) receptors and attenuates dopaminergic supersensitivity. Cyclo(glycyl-L-leucyl) inhibits the development of Morphine induced pain relief as well as dopamine receptor supersensitivity in rats. Cyclo(glycyl-L-leucyl) has the potential for the prevention of tardive and/or L-DOPA (HY-N0304)-induced dyskinesias[1][2].
Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2B receptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility[1][2].
β-Endorphin (rat) is an endogenous opioid neuropeptide and peptide hormone. β-Endorphin (rat) has analgesic activity and also contributes to food intake in satiated rats. β-Endorphin (rat) can be used in the research of neurological diseases such as analgesia and drug addiction[1][2].
Lotilaner is a parasiticide, acts as a potent non-competitive antagonist of insects GABACl receptors, with an IC50 of 23.84 nM for Drosophila melanogaster GABA receptor. No effect on a dog GABAA receptor[1].
FAAH-IN-8 (compound 11) is a competitive inhibitor of FAAH with an IC50 value of 6.7 nM and a Ki value of 5 nM. FAAH-IN-8 has high blood-brain permeability and a significant antioxidant profile with no neurotoxicity[1].
Belaperidone (LU-111995), a 5-HT2A receptor inhibitor, possesses antidopaminergic and antiserotonergic effects[1].
SB 258719 (hydrochloride) is a selective 5-HT7 receptor antagonist displayed high affnity (pKi=7.5) for the receptor. SB-258719 (hydrochloride) can be used for the research of cancer and neurological diseases[1][2].
Xanthotoxol is a biologically active linear furocoumarin, shows strong pharmacological activities as anti-inflammatory, antioxidant, 5-HT antagonistic, and neuroprotective effects.
WAY-100635 maleate is a potent and selective 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 ± 0.12 nM for 5-HT.IC50 Value: 0.95 nMTarget: 5-HT Receptorin vitro: WAY 100635 has an IC50 of 1.35 nM and is > 100-fold selective for the 5-HT1A site relative to a range of other CNS receptors. The Bmax of [3H]WAY 100635 specific binding is consistently 50-60% greater than that of the agonist radioligand, [3H]8-OH-DPAT. Mn2+, but not guanine nucleotides, inhibits [3H]WAY 100635-specific binding. WAY 100635 has no 5-HT1A receptor agonist actions, but dose-dependently blocks the effects of agonists at both the postsynaptic 5-HT1A receptor in the CA1 region of the hippocampus, and the somatodendritic 5-HT1A receptor locates on dorsal raphe 5-HT neurones. [3H]WAY 100635 has a Kd of approximately 2.5 nM. In the isolated guinea-pig ileum WAY 100635 is a potent and, at high concentrations, an insurmountable antagonist of the 5-HT1A receptor agonist action of 5-carboxamidotryptamine, with an apparent pA2 value (at 0.3 nM) of 9.71. in vivo: WAY 100635 blocks the inhibitory action of 8-OH-DPAT on dorsal raphe neuronal firing in the anaesthetised rat at doses which has no inhibitory action per se. In behavioural models, WAY 100635 itself induces no overt behavioural changes but potently antagonises the behavioural syndrome induced by 8-OH-DPAT in the rat and guinea-pig (minimum effective dose = 0.003 mg/kg s.c. and ID50 = 0.01 mg/kg s.c., respectively). WAY 100635 also blocks the hypothermia induced by 8-OH-DPAT in the mouse and rat with ID50 values of 0.01 mg/kg s.c.
Neu2000 is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist.
(R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine[1][2]. (R)-(+)-HA-966 can cross the blood-brain barrier and has the potential for neuropathic and acute pain[3].
Lanicemine (AZD6765) is a low-trapping NMDA channel blocker with a binding (Ki) of 0.56-2.1 μM[1].
NYX-2925 is a Novel NMDA Receptor-Specific Spirocyclic-β-Lactam That Modulates Synaptic Plasticity Processes Associated with Learning and Memory.
Huperzine C is an alkaloid isolated from Huperzia serrate. Huperzine C is an acetylcholinesterase (AChE) inhibotor, with an IC50 of 0.6 μM. Huperzine C can be used for the research of Alzheimer’s Disease[1][2].
Picfeltarraenin IB, a triterpenoid obtained from Picriafel-terrae Lour (P.fel-terrae), is an acetylcholinesterase (AChE) inhibitor. Picfeltarraenin IB can be used for the treatment of herpes infections, cancer and inflammation[1].
Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity[1][2].
AChE/BChE/MAO-B-IN-1 (Compound 10) is a reversible and non-time-dependent AChE, BChE and MAO-B inhibitor with IC50 values of 7.31, 0.56 and 26.1 μM for hAChE, hBChE and hMAO-B, respectively. AChE/BChE/MAO-B-IN-1 can cross the BBB and shows neuroprotective effects without cytotoxicity[1].
6-Aminonicotinic acid is a GABAA receptor agonist with Ki value of 4.4 nM[1].
Risperidone hydrochloride is a serotonin 5-HT2 receptor blocker and a potent dopamine D2 receptor antagonist, with Kis of 0.16, 1.4 nM for 5-HT2 and D2 receptor, respectively.
(Rac)-SEP-363856 is the racemate of SEP-363856. SEP-363856（SEP-856）, an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 （SEP-856） has the potential for the treatment of schizophrenia[1].
MDL 29913, a cyclic pseudopeptide, is a competitive NK2 tachykinin receptor selective antagonist, with a pA2 of 8.66[1].
(S)-UFR2709 is a competitive nAChR antagonist and displays higher affinity for α4β2 nAChRs than for α7 nAChRs. (S)-UFR2709 decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 acts as an anxiolytic agent and can be used for the study of nicotine addiction[1][2].
SCS (Salicylidene salicylhydrazide) is a potent, allosteric and selective inhibitor of β1-containing GABAA receptors with an IC50 of 32 nM against α2β1γ1θ by VIPR measurement. SCS is also a chelator of metal ions[1].
Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia[1][2].