PI3K/Akt/CREB activator 1 (compound AE-18) is a potent, orally active PI3K/Akt/CREB activator. PI3K/Akt/CREB activator 1 promotes neuronal proliferation, induced differentiation of Neuro-2a cells into a neuron-like morphology, and accelerated the establishment of axon-dendrite polarization of primary hippocampal neurons through upregulating brain-derived neurotrophic factor via the PI3K/Akt/CREB pathway. PI3K/Akt/CREB activator 1 can be used in research of vascular dementia (VaD)[1].
3'-O-Methylbatatasin III shows spasmolytic activity[1].
A potent and selective δ-opioid receptor agonist that has high affinity and selectivity for the δ1 subtype with Ki of 1.12 nM; dispalys >1,000-fold selectivity over μOR and κOR; Pain Discontinued
AR-A 2 is a selective 5-HT1B receptor antagonist, with high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guinea pig 5-HT1B receptor; AR-A 2 can be used in the research of depression and anxiety.
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR)[1]. Ro15-4513 is a potent ethanol antagonist[2]. Ro15-4513 has anti-anxiety effect[3].
Tolcapone(Ro 40-7592) is an orally active selective, potent catechol-O-methyltransferase (COMT) inhibitor. IC50 value:Target: COMTTolcapone inhibits both central and peripheral COMT. Tolcapone caused a rapid and reversible inhibition of COMT activity in erythrocytes in parallel with a dose-dependent decrease in the formation of 3-OMD. Tolcapone increased the area under the concentration-time curve and elimination half-life of levodopa. Tolcapone crosses the blood-brain barrier, and has been used for L-DOPA adjunct therapy in the treatment of Parkinson's disease.
Peucedanocoumarin III is an inhibitor of (alpha)-synuclein and Huntington protein aggregates that enhances the clearance of nuclear and cytoplasmic β23 aggregates and prevents cytotoxicity induced by disease-associated proteins (i.e., mutant Huntington proteins and α-synuclein). Peucedanocoumarin III may be used in Parkinson's disease research[1].
WAY-620147 (compound 6) is an N-(2-morpholinoethyl)nicotinamide derivative that inhibits monoamine oxidase (Monoamine Oxidase). WAY-620147 inhibits MAO-A and MAO-B with IC50s of 26 μM and 55 μM, respectively[1].
Isopteropodine is heteroyohimbine-type oxindole alkaloid components of Uncaria tomentosa (Willd.) DC. Isopteropodine acts as positive modulators of muscarinic M1 and 5-HT2 receptors[1].
hMAO-B-IN-4 (compound B10) is a selective, reversible and blood–brain barrier (BBB) penetrable human monoamine oxidase-B (hMAO-B) inhibitor with an IC50 value and a Ki value of 0.067 and 0.03 μM, respectively. hMAO-B-IN-4 inhibits hMAO-A with an IC50 value of 33.82 μM. hMAO-B-IN-4 can be used for Alzheimer’s disease (AD) and Parkinson’s disease (PD) research[1].
Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions[1].
Stromatoxin 1 is an inhibitor of Potassium Channel, a peptide which can be isolated from tarantulas. Stromatoxin 1 selectively inhibits K(V)2.1, K(V)2.2, K(V)4.2, and K(V)2.1/9.3 channels. K(V)2.1 and K(V)2.2, but not K(V)4.2, channel subunits play a key role in opposing both myogenic and neurogenic urinary bladder smooth muscle (UBSM) contractions in rats[1].
ML351 is a potent and highly specific 15-LOX-1 inhibitor with an IC50 of 200 nM. ML351 shows excellent selectivity (>250-fold) versus the related isozymes, 5-LOX, platelet 12-LOX, 15-LOX-2, ovine COX-1, and human COX-2[1]. ML351 prevents dysglycemia and reduces β-cell oxidative stress in nonobese diabetic mouse model of T1D[2].
TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC50=1μM; Kd= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity[1].
Protriptyline is a potent antidepressant agent. Protriptyline inhibits AChE activity with IC50 value of 0.06 mM and inhibits Aβ Self-Assembly. Protriptyline can be used for depression and Alzheimers disease[1][2][3].
NBQX disodium (FG9202 disodium) is a highly selective and competitive AMPA receptor antagonist. NBQX disodium has neuroprotective and anticonvulsant activity[1].
SKF 82958 is a D1/D5 receptor full agonist. IC50 value:Target: D1/D5 receptorin vitro: Neuropeptide and immediate early gene expression in striatonigral neurons of the normosensitive striatum is induced by mixed D1 receptor SKF-82958, which induces behavioral activity and preprodynorphin (PPD) and substance P (SP) gene expression in medium spiny neurons in the dorsal, and especially, in the ventral striatum. in vivo:Quantitative in situ hybridization was used to examine the contribution of muscarinic receptors to the transynaptic regulation of striatal gene expression induced by D1receptor activation. The acute injection of the full D1 agonist, SKF-82958, would induce PPD, SP and PPE mRNA expression in the intact rat striatum.
Cbz-Pro-Leu-Gly-OH is a tripeptide that can be used in Parkinson's disease research[1].
Analgesic agent-3 (compound 3d) is a potent analgesic agent[1].
Fluoroethylnormemantine hydrochloride, a derivative of Memantine, is an antagonist of the N-methyl-D-aspartate (NMDA) receptor. [18F]-Fluoroethylnormemantine hydrochloride can be used as a positron emission tomography (PET) tracer. Fluoroethylnormemantine hydrochloride exhibits anti-amnesic, neuroprotective, antidepressant-like and fear-attenuating effects[1][2][3].
Ethyl dirazepate is a drug which is a benzodiazepine derivative. It has anxiolytic and hypnotic and possibly other characteristic benzodiazepine properties.
Amyloid β-peptide (1-40) (rat) is the prone-to-aggregation product of amyloid precursor protein proteolytic cleavage, and is the major constituent of senile plaques observed in the brain of Alzheimer’s disease.
CP 93129 dihydrochloride is a potent 5HT1B receptor agonist. CP 93129 dihydrochloride has the potential for parkinson's disease research[1].
Nalfurafine (TRK-820) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential[1]. Nalfurafine (TRK-820) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment[2].
Glycine-1-13C,15N is the 13C- and 15N-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
BAN ORL 24 is a potent and selective NOP receptor antagonist. (IC50 values are 0.27, 2500, 6700 and > 10000 nM for NOP, κ-, μ- and δ-receptors respectively). IC50 value: 0.27 nMTarget: NOP receptorBAN ORL 24 inhibits nociceptin-induced stimulation of [35S]-GTPγS binding and Ca2+ mobilization in CHO cells in vitro. BAN ORL 24 antagonizes NOP agonist-induced reduction in locomotor activity in vivo. Brain penetrant.
CART(55-102)(human) is an endogenous satiety factor with potent appetite-suppressing activity. CART(55-102)(human) is closely associated with leptin and neuropeptide Y[1][2].
Rp-cAMPS, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS is resistant to hydrolysis by phosphodiesterases[1][2][3][4][5][6].
A-317567 is a potent acid-sensing ion channel 3 (ASIC-3) inhibitor with an IC50 of 1.025 μM. A-317567 has antidepressant and antinociception effects[1][2].
LY 344864 hydrochloride is a selective 5-HT1F agonist with a Ki of 6 nM.