6,2'-Dihydroxyflavone is a novel antagonist of GABAA receptor.
NPS ALX Compound 4a is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist with an IC50 of 7.2 nM, which also has a great binding affinity with Ki of 0.2 nM[1].
Ro19-4603 is a benzodiazepine inverse agonist. Ro19-4603 antagonizes ethanol (EtOH) intake in alcohol-preferring rats[1].
RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.
Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
MRK-898 is an orally active GABA(A) receptor modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with Ki values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s)[1].
AMG-8718 is a potent, selective and orally active BACE1 inhibitor with IC50 values of 0.0007, 0.005 µM for BACE1 and BACE2, respectively. AMG-8718 significantly decreases Aβ40 levels in the CSF and brain[1].
D-Tetrahydropalmatine is an isoquinoline alkaloid, mainly in the genus Corydalis[1]. D-Tetrahydropalmatine is a Dopamine (DA) receptor antagonist with preferential affinity toward the D1 receptors[2]. D-Tetrahydropalmatine is a potent organic cation transporter 1 (OCT1) inhibitor[3].
Oxantel (CP-14445), a m-oxyphenol derivative of Pyrantel (HY-12641), is a N-subtype AChR agonist. Oxantel is an anthelmintic, with excellent trichuricidal properties[1][2].
A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM)[1].
Quetiapine D4 fumarate is the deuterium labeled Quetiapine, which is an atypical antipsychotic.
SKF89976A hydrochloride is a selective GABA transporter (GAT-1) inhibitor with IC50s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.
Benzoctamine hydrochloride (Ba-30803) is a psychoactive agent with anti-anxiety effect. Benzoctamine hydrochloride blocks the central postsynaptic serotonin receptors and decreases 5-HT turnover in the brain[1][2].
[Lys5,MeLeu9,Nle10]-NKA(4-10) is a highly selective and potent NK2 receptor agonist, with an IC50 of 6.1 nM[1].
Clothiapine, an atypical antipsychotic agent, shares with clozapine its strong antiserotonergic properties[1].
Pindolol-d7 (LB-46-d7) is the deuterium labeled Pindolol. Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33 nM)[1][2].
NGB 2904 is an orally active and selective dopamine (DA) D3 receptor antagonist. NGB 2904 can be used for the research of cocaine addiction[1].
U92016A hydrochloride is a potent, metabolically stable, orally acitive 5-HT1A receptor agonist with an exceptionally high degree of intrinsic activity[1][2]. U92016A hydrochloride binds with high affinity to human 5-HT1A receptors expressed in Chinese hamster ovary cells (Ki=0.2 nM)[2].
Dihydrexidine hydrochloride (DAR-0100 hydrochloride) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist, with an IC50 of 10 nM for D1 receptor. Dihydrexidine hydrochloride exhibits potent antiparkinsonian activity[1][2][3][4].
MAO-B-IN-12 (Compound 16c) is a potent monoamine oxidase B (MAO-B) inhibitor with an IC50 of 1.3 μM. MAO-B-IN-12 shows a neuroprotective activity[1].
Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C[1][2].
Dopamine D3 receptor ligand-4 (compound 6) is a potent and selective dopamine D3 receptor ligand, with a Ki of 0.5 nM. Dopamine D3 receptor ligand-4 shows high level of selectivity for D3 over D2 (Ki=7.43 nM). Dopamine D3 receptor ligand-4 can be used for the research of Cocaine use disorder[1].
SB269970 hydrochloride is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.IC50 Value: 8.3 (pKi for 5-HT7) [1]Target: 5-HT7 receptorin vitro: 5-CT-stimulated adenylyl cyclase activity in guinea-pig hippocampal membranes (pEC(50) of 8.4+/-0.2) was inhibited by SB-269970-A (0.3 microM) with a pK(B) (8.3+/-0.1) in good agreement with its antagonist potency at the human cloned 5-HT(7(a)) receptor and its binding affinity at guinea-pig cortical membranes. 5-HT(7) receptor mRNA was highly expressed in human hypothalamus, amygdala, thalamus, hippocampus and testis [1]. Cortical slices were loaded with [(3)H]-5-HT and release was evoked by electrical stimulation. 5-CT inhibited the evoked release of [(3)H]-5-HT in a concentration-dependent manner. SB-269970 had no significant effect on [(3)H]-5-HT release while the 5-HT(1B) receptor antagonist, SB-224289 significantly potentiated [(3)H]-5-HT release. In addition, SB-269970 was unable to attenuate the 5-CT-induced inhibition of release while SB-224289 produced a rightward shift of the 5-CT response, generating estimated pK(B) values of 7.8 and 7.6 at the guinea-pig and rat terminal 5-HT autoreceptors respectively [2].in vivo: Acute administration of SB-269970 (1 mg/kg) or amisulpride (3 mg/kg) ameliorated ketamine-induced cognitive inflexibility and novel object recognition deficit in rats. Both compounds were also effective in attenuating ketamine-evoked disruption of social interactions [3]. Pretreatment with a dose of SB-269970 (0.5 mM) that significantly affects sleep variables antagonized the LP-44 (2.5 mM)-induced suppression of REMS and of the number of REM periods [4].Toxicity: N/AClinical trial: N/A
F 14679 is a prototypical 5-HT1A agonist with a pKi of 10.23. F 14679 induces large Ca2+ responses[1].
Isonipecotic acid-d9 is the deuterium labeled Isonipecotic acid[1]. Isonipecotic acid is a GABAA receptor partial agonist[2].
Anabaseine, an alkaloid, stimulates a wide variety of animal nicotinic acetylcholine receptors (AChRs), especially the neuromuscular receptors and α7 AChRs[1].
[Leu5]-Enkephalin, amide is a δ opioid receptor agonist.
Etomidate Hcl(R16659 Hcl) is a GABAA receptors agonist, which is a short acting intravenous anaesthetic agent used for the induction of general anaesthesia.Target: GABA ReceptorEtomidate is a potent inhibitor of the adrenal response to surgery. The absence of clinical consequences associated with the blunted response suggests that a major increase in adrenal hormone production may not be necessary during surgery [1]. Etomidate is an intravenous induction agent that is associated with hemodynamic stability during intubation. The agent is therefore attractive for use in critically ill patients who have a high risk of hemodynamic instability during this procedure [2]. Etomidate use was not associated with all cause 28-day mortality or hospital mortality but was associated with significantly higher ICU mortality (91% vs. 64% for etomidate and controls groups, respectively; p = 0.02). Etomidate patients who received subsequent doses of hydrocortisone required lower doses of vasopressors and had more vasopressor-free days but no improvement in mortality [3].Clinical indications: FDA Approved Date: 1983Toxicity: Undesirable side effects of etomidate that may limit its use include pain on injection, myoclonus and adrenocortical suppression lasting 4-6 hours following an induction dose.
RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites[1].
Domoic acid ((-)-Domoic acid; L-Domoic acid) is an excitatory neurotransmitter isolated from a form of marine vegetation, Nitzschia pungens[1]. Domoic acid produces neurotoxic effect through activating kainate receptor[2].