Propofol-d17 (2,6-Diisopropylphenol-d17) is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic[1].
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes[1][4]. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro[2]. AZD7325 has the potential for the investigation of anxiety and dravet syndrome[3]. PAM: positive allosteric modulator.
GR 94800 is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively[1][2].
O-GlcNAcase-IN-4 is a O-GlcNAcase inhibitor extracted from patent WO2018140299A1 Formulaic Ic. O-GlcNAcase-IN-4 can be used for the research of neurodegenerative diseases and disorders, such as Alzheimer's disease[1].
μ opioid receptor agonist 1 （Compound H-1a）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].
Trazodone HCl is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders.Target: 5-HT ReceptorTrazodone is a triazolopyridine derivative, chemically and pharmacologically unrelated to other currently available antidepressants. Trazodone has been successfully used in a small number of patients with depression and pre-existing cardiovascular disease. trazodone has also been used as a hypnotic for psychotropic-induced or other insomnias with some success [1]. Trazodone is an effective hypnotic for patients with antidepressant-associated insomnia [2]. Trazodone may be helpful in men with erectile dysfunction (ED), possibly more so at higher doses, and in men with psychogenic ED. Future high-quality trials should compare trazodone with placebo and other therapies in men with depression and psychogenic ED [3].
N-type calcium channel blocker-1 is an orally active analgesic agent which shows high affinity to functionally block N-type calcium channels with an IC50 of 0.7 μM in the IMR32 assay.
SNC162 is a delta-opioid receptor agonist with an IC50 of 0.94 nM. SNC162 has antidepressant-like effects and produces a selective enhancement of the antinociceptive effects of fentanyl in rhesus monkeys[1][2].
5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.
R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils[1][2][3][4].
CP-113818 is a potent cholesterol acyltransferase (ACAT) inhibitor. CP-113818 can be used for the research of Alzheimer's disease[1].
TTA-Q6 is a selective T-type Ca2+ channel antagonist, used in the neurological disease.
Pinoresinol dimethyl ether ((+)-Eudesmin) is a non-phenolic furofuran lignan isolated from the stem bark of Magnolia kobus with neuritogenic activity. Pinoresinol dimethyl ether ((+)-Eudesmin) can induce neuritis outgrowth from PC12 cells by stimulating up-stream MAPK, PKC and PKA pathways[1][2].
(RS)-AMPA ((±)-AMPA) is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA does not interfere with binding sites for kainic acid or NMDA receptors[1][2].
Calycanthine, the principal alkaloid of the order Calycanthaceae, has been isolated from a species of the genus Psychotria, and is a central nervous system toxin, causing convulsions[1][2].
Tryptamine-d2 hydrochloride is a deuterium labeled Tryptamine hydrochloride. Tryptamine hydrochloride is a monoamine alkaloid, similar to other trace amines, is believed to play a role as a neuromodulator or neurotransmitter[1].
Morphiceptin is a potent and specific agonist for morphine (μ) receptors. Morphiceptin, as a synthetic peptide, is the amide of a fragment of the milk protein β-casein. Morphiceptin has morphinelike activities and is highly specific for morphine (μ) receptors but not for enkephalin (⸹) receptors[1].
Ropivacaine HCl is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.Target: Sodium ChannelRopivacaine is a new long-acting local anesthetic, with vasoconstrictive properties. Ropivacaine given epidurally provided adequate sensory anesthesia and motor block for transurethral surgery. Addition of epinephrine did not provide any significant prolongation of the sensory or motor block, nor any influence upon the sympathetic block [1]. Ropivacaine was metabolized to 2',6'-pipecoloxylidide (PPX), 3'-hydroxyropivacaine (3'-OH Rop), and 4'-hydroxyropivacaine (4'-OH Rop) by hepatic microsomes from human and rat. Ropivacaine N-dealkylation and 3'-hydroxylation activities correlated well with the level of CYP3A4 and 1A2 in human hepatic microsomes, respectively [2].
β-FXR antagonist 1 (C 12), an isomer of FXR antagonist 1 (HY-151481) is a FXR antagonist[1].
Methyl isoeugenol (MIE) is a natural food flavour that can be isolated from Pimenta pseudocaryophyllus leaf. Methyl isoeugenol shows anxiolytic and antidepressant like effects. Methyl isoeugenol is orally active[1].
CyPPA is a positive modulator of hSK3 and hSK2, with EC50 values of 14 μM and 5.6 μM, repectively. CyPPA is inactive on both hSK1 and hIK channels[1][2].
Zuclopenthixol is a thioxanthene derivative which acts as a mixed dopamine D1/D2 receptor antagonist.
LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.IC50 Value: 6 nM (Ki) [1]Target: 5-HT1FLY344864 possesses little affinity for the 56 other serotonergic and non-serotonergic neuronal binding sites examined [1].in vitro: he 5-HT1A, 5-HT1B and 5-HT1D receptor agonists 8-OH-DPAT (3 microM), CP93129 (3 microM) and L694247 (3 microM), but not the 5-HT1F receptor agonist LY344864 (1 - 3 microM) inhibited evoked IPSCs [2].in vivo: After an intravenous dose of 1 mg/kg, rat plasma LY344864 levels declined with time whereas brain cortex levels remained relatively constant for the first 6 hours after injection. Oral and intravenous LY344864 administration potently inhibited dural protein extravasation caused by electrical stimulation of the trigeminal ganglion in rats [1]. Sumatriptan, zolmitriptan, rizatriptan, and naratriptan all contracted the rabbit saphenous vein from baseline tone, whereas LY344864 in concentrations up to 10(-4) M did not contract the rabbit saphenous vein. Furthermore, vascular contractions to sumatriptan were markedly augmented in the presence of prostaglandin F(2alpha) (PGF(2alpha)). However, even in the presence of PGF(2alpha) (3 x 10(-7) M), LY344864 did not contract the rabbit saphenous vein in concentrations well in excess of its 5-HT(1F) receptor affinity (pK(i) = 8.2) [3].
Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic.
(RS)-CPP ((±)-CPP) is a potent and selective NMDA antagonist. (RS)-CPP inhibits central neuron responses, and has anticonvulsant activity[1].
N6-Benzyl-5'-ethylcarboxamido adenosine is a selective A3 adenosine receptor agonist[1].
A novel potent and selective negative modulator of AMPA receptors containing TARP-gamma8
ASP 2905 (ASP2905) is a novel potent, selective, orally bioavailable inhibitor of voltage-gated potassium channel KCNH3 with IC50 of 9.0 nM; displays minimally bound with low affinities to 55 transmembrane proteins; decreases the frequency of spontaneous inhibitory postsynaptic currents in cultured rat hippocampal neurons at 0.1-1 uM; reverses the disruption of spontaneous alternation behavior induced by MK-801 and scopolamine in mice, and ameliorates the cognitive deficits of aged rats. Alzheimer Disease Phase 1 Discontinued
hBChE-IN-2 (compound 15d) is a butyrylcholinesterase (BChE) inhibitor (IC50 of 0.62 μM) and a cannabinoid receptor 2 (CB2R) agonist. hBChE-IN-2 has neuroprotection activities[1].
Aβ42-IN-2 is a γ-secretase modulators extracted from patent WO2016070107, compound example example 36. Aβ42-IN-2 has an IC50 of 6.5 nM for Αβ42. Aβ42-IN-2 can be used for the research of a disorder associated with aberrant A3 peptide levels, including Alzheimer's disease[1].