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].
Muscarine ((+)-Muscarine) tosylate is an agonist of prototype mAChR. Muscarine tosylate is a toxin that can stimulate the parasympathetic nervous system[1][2].
Thymopoietin i/ii (29-41) (bovine) is a peptide corresponding to positions 29-41 of bovine thymopoietin II. Thymopoietin i/ii (29-41) (bovine) is a neuromuscular blocker[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].
Radafaxine ((S,S)-Hydroxybupropion) is an antidepressant. Radafaxine blocks dopamine transporters (DAT). Radafaxine is an active metabolite of Bupropion[1][2].
Cyclophostin is an acetylcholinesterase (AChE) inhibitor with IC50 values of 45, 0.76 and 1.3 nM for humans and two different insects, respectively[1].
Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 and 1.5μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1[1][2][3][4].
Emicerfont is a corticotropin-releasing factor type 1 (CRF1) receptor antagonist with an IC50 of 66 nM.
NEP (VDP-green (NEP)) is a turn-on fluorescent probe based on the intramolecular charge transfer (ICT) mechanism for sensing vicinal dithiol-containing proteins (VDPs). NEP is exhibits high selectivity toward VDPs in live cells and in vivo and displays a strong green fluorescence signal (λex/λem=430/535 nm). NEP has the potential for parkinsonism[1].
Prothipendyl hydrochloride is an orally active agent that can be used in the study of mental symptoms in the aged (e.g. anxiety)[1].
(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].
(±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist with a Ki of 1.8 nM for cloned human ORL1. J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC50 value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin/orphanin FQ[1].
[Sar9,Met(O2)11]-Substance P is a tachykinin NK1 receptor selective agonist.
Benperidol is a relatively old antipsychotic drug. Benperidol is a butyrophenone antipsychotic, with the highest neuroleptic potency in terms of D2 receptor blockade[1].
DU125530 is a potent and selective5-HT1A receptor antagonist with Ki values of 0.7, 890, 1200, 240, 750, 1100 nM for 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2C, 5-HT3, respectively. DU125530 shows antidepressant effects[1][2].
Gomisin M2 ((+)-Gomisin M2) is a lignan isolated from the fruits of Schisandra rubriflora with anti-HIV activity (EC50 of 2.4 μM). Gomisin M2 exhibits anti-cancer and anti-allergic activities and has the potential for Alzheimer’s disease research[1][2].
PF-03654764 is an orally active, selective histamine H3 receptor antagonist with Ki values of 1.2 nM and 7.9 nM for human H3 and rat H3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research[1][2].
URMC-099 is an orally bioavailable and potent mixed lineage kinase type 3 (MLK3) (IC50=14 nM) inhibitor with with excellent blood-brain barrier penetration properties.
Docosahexaenoic acid ethyl ester (Ethyl docosahexaenoate) is a 90% concentrated ethyl ester of docosahexaenoic acid manufactured from the microalgal oil. Docosahexaenoic acid ethyl ester enhances 6-hydroxydopamine-induced neuronal damage by induction of lipid peroxidation in mouse striatum. Docosahexaenoic acid (DHA) is a key component of the cell membrane, and its peroxidation is inducible due to the double-bond chemical structure. Docosahexaenoic acid has neuroprotective effects[1][2].
RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 reduces alcohol reinforcement and intake behaviors in rats[1].
SX-3228 is a selective benzodiazepine1 (BZ1) receptor agonist with an IC50 of 17 nM.
Phenyltoloxamine (Bistrimin) is an antihistamine agent with sedative and analgesic effects. Phenyltoloxamine also has potent Sigma-1 receptor binding affinity (Ki: 160 nM)[1][2][3].
Itruvone is a intermediate of 17α-ethinylestradiol (EE2) during Fenton oxidation. Itruvone has an antidepressant effect[1][2].
Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects[1][2][3].
GB83 is a potent PAR2 antagonist. GB83 reverses neutrophil elastase‐induced synovitis and pain. GB83 blocks the effect of MET-1 supernatant on NG neurons[1].
PF-04885614 is a potent NaV1.8 inhibitor, extracted from patent US2018328915. PF-04885614 has potential for neurological and neurodevelopmental diseases treatment[1].
Bavisant (JNJ-31001074) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. IC50 Value: Target: H3 receptorin vitro: Bavisant completed a phase II ADHD trial, but no results have been reported [1].in vivo: Mean change from baseline in the total ADHD-RS-IV score at day 42 (primary efficacy endpoint) was -8.8 in the placebo group versus -9.3, -11.2 and -12.2 in the bavisant 1?mg/day, 3?mg/day and 10?mg/day groups, respectively; the change in the 10?mg/day group was not statistically superior to placebo (p=0.161), and hence statistical comparisons of the 1?mg/day and 3?mg/day groups with placebo based on a step-down closed testing procedure were not performed [2].Clinical trial: A Study to Characterize the Pharmacokinetics and Effect of Food on JNJ-31001074 in Healthy Volunteers. Phase 2