S1R agonist 1 (Compound 6b) is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity[1].
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes[1][2][3][4].
(2R,4R)-APDC is a selective group II metabotropic glutamate receptors (mGluRs) agonist. (2R,4R)-APDC has anticonvulsant and neuroprotective effects[1][2].
GPR139 agonist-2 (compound 20a) is a potent GPR139 agonist with an EC50 of 24.7 nM. GPR139 agonist-2 rescues the social interaction deficits and alleviates cognitive deficits in murine schizophrenia models. GPR139 agonist-2 has the potential for antischizophrenia drug research[1].
Verubecestat (MK-8931) is a beta-secretase 1 (BACE1) inhibitor under investigation for the treatment of Alzheimer's Disease.
6,2'-Dihydroxyflavone is a novel antagonist of GABAA receptor.
MEHFPGP is a nootropic neuroprotective peptide. MEHFPGP can be used in the research of brain stroke[1][2].
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].
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].
GW542573X is a potent and selective Ca2+-activated K+ 2 (SK2) channels activator. GW542573X induces the Ca2+-response curve of hSK1 that left-shifted from an EC50 (Ca2+) value of 410 nM to 240 nM[1].
SOMCL-668 is a selective and potent sigma-1 receptor allosteric modulator. ?SOMCL-668 shows positive modulation of improvement in social deficits and cognitive impairment induced by the selective sigma-1 agonist PRE084.?SOMCL-668 displays anti-seizure activities and can be used for psychotic illness research[1].
Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII) with nematicidal properties. Conoidin A covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC50 of 23 µM. Conoidin A also inhibits hyperoxidation of mammalian PrxI and PrxII (but not PrxIII)[1][2]. Conoidin A has antioxidant, neuroprotective effects and can be used for the research of ischaemic heart disease[3].
Tomatine is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.). Tomatine elicits neurotoxicity in RIP1 kinase and caspase-independent manner. Tomatine promotes the upregulation of nuclear apoptosis inducing factor (AIF) in neuroblastoma cells. Tomatine also inhibits 20S proteasome activity[1].
APETx2, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain[1][2].
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
β-Caryophyllene is a CB2 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.
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].
PD 119819 is a highly selective benzopyran-4-one brain dopamine autoreceptor agonist. PD 119819, a heterocyclic piperazine, inhibits spontaneous locomotor activity and brain dopamine synthesis[1][2].
6-Iodoamiloride is a potent acid-sensing ion channel 1 (ASIC1) inhibitor with an IC50 of 88 nM. 6-Iodoamiloride inhibits ASIC3-mediated currents from rat dorsal root ganglion neurons with an IC50 of 230 nM[1].
VUF10166 is a potent and high-affinity 5-HT3 receptor antagonist, with Ki values of 0.04 nM (5-HT3A) and 22 nM (5-HT3AB). VUF10166 inhibits 5-HT-induced responses at 5-HT3A and 5-HT3AB receptors at nanomolar concentrations. At 5-HT3 receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC50 of 5.2 μM[1].
(R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol (HY-B0573). Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1].
Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM[1].
Cerebroside A is a single molecule cerebroside extracted and isolated from an edible mushroom. Cerebroside A provides potent neuroprotection after cerebral ischaemia through reducing glutamate release and Ca²⁺ influx of NMDA receptors[1].
SM-2470 is a potent α1-adrenoceptor antagonist, has sympathetic nerve activity in anesthetized rats[1]. SM-2470 is an antihypertensive agent. SM-2470 exhibits hypocholesterolaemic effect by the inhibition of cholesterol absorption related to the reduction of cholesterol solubilization[2].
A novel potent, selective PDE9A inhibitor with IC50 of 11 nM, >45-fold selectivity over other PDE isoforms; shows better selectivity than (R)-C33 against PDE5.
Clocinnamox (mesylate) is a potent opioid antagonist acting at mu, kappa and delta-receptors. Clocinnamox is a selective mu-receptor antagonist than kappa and delta-receptors[1].
2-Iminobiotin (Guanidinobiotin) is a biotin (vitamin H or B7) analog. 2-Iminobiotin is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5μM for murine iNOS and rat n-cNOS, respectively[1]. 2-Iminobiotin superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage[2].
CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist (Ki=1.2 nM; EC50=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties[1][2].