(2S,3S)-E1R (Compound 2d) is an enantiomer of E1R. (2S,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders[1].
(-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.
Propantheline bromide is an antimuscarinic agent, used for the treatment of hyperhidrosis, cramps or spasms of the stomach, intestines or bladder, and enuresis.
Sacubitrilat is an active neprilysin (NEP) inhibitor.
Zatosetron maleate is a potent and selective 5HT3 receptor antagonist.
Propanidid (Sombrevin; Fabantol) is a γ-aminobutyric acid type A (GABAA) receptor agonist and a short-acting non-barbiturate general anesthetic agent. Propanidid can decrease the arterial pressure[1][2].
(-)-Rabdosiin is a novel phenolic marker, found from Symphytum officinale L. (-)-Rabdosiin shows antioxidant, neuroprotective or anti-HIV activities[1].
QNZ46 is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist (IC50 values are 3, 6, 229, and >300, >300 μM for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively). IC50 value: 3 μM (for NR2D), 6 μM (for NR2C), 229 μM (for NR2D NR2A)Target: NR2D, NR2C, NR2Ain vitro: QNZ46 is a noncompetitive inhibitor of GluN2C/D containing NMDA receptors. KD and IC50 values for binding and inhibition of GluN1/Glun2D receptors by QNZ46 are 4.9 and 3.9 μM, respectively. QNZ46 does not compete for binding of glutamate or glycine, but QNZ46 receptor binding requires the binding of glutamate to the GluN2 subunit.
Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy[1][2][3].
5α-Androstane-3β,5,6β-triol is a neuroprotectant. 5α-Androstane-3β,5,6β-triol can remarkably reverse intracellular acidification and alleviate neuronal injury through the inhibition of AMPK signaling. 5α-Androstane-3β,5,6β-triol remarkably reduced the infarct volume and attenuated neurologic impairment in acute ischemic stroke models of middle cerebral artery occlusion in vivo[1].
Elenbecestat (E2609) is a novel potent BACE-1 inhibitor for the treatment of Alzheimer's disease (AD)[1].
Fosaprepitant (L-758298) is a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.IC50 Value:Target: NK1 receptorin vitro: Fosaprepitant (also known as MK-0517 and L-758,298) is a water-soluble phosphoryl prodrug for aprepitant, which, when administered intravenously, is converted to aprepitant within 30 min of intravenous administration via the action of ubiquitous phosphatases. Owing to the rapid conversion offosaprepitant to the active form (aprepitant), fosaprepitant 115 mg provided the same aprepitant exposure in terms of AUC as aprepitant 12 mg orally, and fosaprepitant is expected to provide a correspondingly similar antiemetic effect as aprepitant [1]. in vivo: Fosaprepitant is well tolerated with mild to moderate venous irritation being the only additional toxicity to those seen with oral aprepitant, and that is a function of dose, concentration, and infusion rate [2]. Patients receiving cisplatin ≥ 70 mg/m(2) for the first time received ondansetron and dexamethasone with a standard aprepitant regimen (125 mg on day 1, 80 mg on day 2, 80 mg on day 3) or a single-dose fosaprepitant regimen (150 mg on day 1) [3]. Single-dose fosaprepitant used in combination with granisetron and dexamethasone was well-tolerated and effective in preventing chemotherapy-induced nausea and vomiting in patients receiving highly emetogenic cancer chemotherapy, including high-dose cisplatin [4].
Mosapramine (Clospipramine) is an orally active and potent dopamine receptor antagonist with high affinity to dopamine receptor subtypes 2, 3 and 4, and with moderate affinity for the 5-HT2 receptor. Mosapramine shows antipsychotic activity and can be used in schizophrenia research[1][2].
PE154 (Compound 13) is a potent fluorescent inhibitor of human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (IC50s=280 pM and 16 nM, respectively)[1]. PE154 can label β-amyloid plaques in histochemical analysis[2].
Landipirdine is a selective antagonist of 5-HT6R. Landipirdine has great effect on the hERG pharmacophore[1].
Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research[1][2][3][4].
F992 is an antidiuretic peptide and vasopressin (antidiuretic hormone) analogue[1].
Calcitonin gene-related peptide (CGRP) is a neuropeptide. Calcitonin gene-related peptide can be used for the research of nociception, ingestive behaviour and modulation of the endocrine systems[1].
Threo-dihydrobupropion is a major metabolite of Bupropion, formed via oxidation and reduction exhibit pharmacological activity. Bupropion, a dual dopamine-norepinephrine uptake inhibitor and a nicotine receptor antagonist, is widely used in the management of depression and as a smoking cessation aid[1].
PF-05085727 is a potent, selective and brain penetrant Phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 2 nM.
(S)-SBFI-26 is the (S) enantiomer of SBFI-26, an anti-nociceptive agent binds to anandamide transporters FABP5 and FABP7. (S)-SBFI-26 has anti-nociceptive and anti-inflammatory effects[1].
Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.
BChE/HDAC6-IN-1 is a potent and selective dual BChE/HDAC6 inhibitor with IC50 values of 4 and 8.9 nM, respectively. BChE/HDAC6-IN-1 ameliorates the cognitive impairment in an Aβ1–42-induced mouse model and has the potental for AD research[1].
1,3,5-Trimethoxybenzene is a key component of the Chinese rose odor. 1,3,5-Trimethoxybenzene is synthesized in three successive methylation steps from phloroglucinol, the initial precursor. 1,3,5-Trimethoxybenzene is an effective sedative[1].
6,4'-Dihydroxy-7-methoxyflavanone, a flavonoid, is a nature product that could be isolated from Heartwood Dalbergia odorifera. 6,4'-Dihydroxy-7-methoxyflavanone inhibits receptor activators of nuclear factor kappa-B ligand (RANKL) induced osteoclastogenesis. 6,4'-Dihydroxy-7-methoxyflavanone has antioxidant, anti-inflammatory and neuroprotective effects. 6,4'-Dihydroxy-7-methoxyflavanone can be used in research of osteoporosis[1].
THK-5117, an arylquinoline derivative, displays high binding affinity to tau fibrils with a Ki of 10.5 nM. THK-5117 has high binding affinity to tau protein aggregates and tau-rich Alzheimer disease (AD) brain homogenates. 18F-THK-5117 has the potential to act as a tau imaging PET probe[1].
Emicerfont is a corticotropin-releasing factor type 1 (CRF1) receptor antagonist with an IC50 of 66 nM.
(Rac)-TTA-P2 is the inactive isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease[1].
L-Histidine-13C6,15N3 is 13C and 15N-labeled L-Histidine (HY-N0832). L-Histidine is an essential amino acid for infants. L-Histidine is an inhibitor of mitochondrial glutamine transport.
γ-Secretase modulator 12 (Compound 1a) is a γ-secretase modulator that can selectively decrease amyloid-β42 (Aβ42) levels (IC50 of 0.39 µM). γ-Secretase modulator 12 can be used for Alzheimer’s disease research. γ-Secretase modulator 12 has a good brain/plasma ratio (Kp, brain = 0.72) in mice[1].