Neurotransmission, neural targets and neurological research.
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CAS 26921-17-5
(S)-Timolol maleate, is a potent non-selective β-adrenergic receptor antagonist (Ki values are 1.97 and 2.0 nM for β1 and β2 receptor subtypes respectively).(S)-Timolol, 50% bioavailability following oral administration. Does not cross the blood brain…
CAS 773092-05-0
Acotiamide monohydrochloride trihydrate is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia. Acotiamide monohydrochloride trihydrate enhances acetylcholine released by enteric neurons through muscarinic…
CAS 103429-31-8
CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor…
CAS 95635-56-6
Ranolazine(RS-43285) is an antianginal agent with antiarrhythmic properties that achieves its effects via a novel mechanism of action (inhibition of the late phase of the inward sodium current), without affecting heart rate or blood pressure (BP).Ranolazine…
CAS 1060461-67-7
NUCC-0200590 is a small-molecule inhibitor of the TRIP8b-HCN interaction with IC50 of 7.0 uM in AlphaScreen assays, effectively disrupts the TRIP8b-HCN interaction in vitro and in vivo.
CAS 1353979-43-7
NMDAR/TRPM4 inhibitor 8 (Compound 8) is a neuroprotective NMDAR-TRPM4 interaction interface inhibitor but spare the critical healthy NMDAR function.
CAS 1259305-29-7
Aripiprazole lauroxil, an N-acyloxymethyl prodrug of aripiprazole, is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia. Aripiprazole lauroxil is cleaved by body’s enzyme esterase to N-hydroxymethyl aripiprazole (plus lauric acid) and…
CAS 635323-95-4
F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM.
CAS 106266-06-2
Risperidone(Risperdal) is an atypical antipsychotic used to treat schizophrenia (including adolescent schizophrenia), schizoaffective disorder, the mixed and manic states associated with bipolar disorder, and irritability in children with autism. This drug…
CAS 61477-94-9
Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.
CAS 4430-36-8
Erucin is a sulforaphane analog and telomerase inhibitor found in cruciferous vegtables. It induces phase II enzyme activity, suppresses cellular proliferation in hepatocellular carcinoma cells, prevents 6-OHDA-induced neurodegenration, and inhibits…
CAS 2244614-14-8
BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.BTRX-335140 endows with favorable in vitro ADMET…
CAS 60142-96-3
Gabapentin (Neurontin) is a pharmaceutical drug, specifically a GABA analog. It was originally developed to treat epilepsy, and currently is also used to relieve neuropathic pain.
CAS 120011-70-3
Donepezil Hcl(E-2020) is a noncompetitive acetylcholinesterase inhibitor, which can readily cross the blood brain barrier and increases the concentration of cortical acetylcholine.It is known that Donepezil Hydrochloride is a useful tool in the study of…
CAS 132112-35-7
Ropivacaine HCl is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.Ropivacaine is a new long-acting local anesthetic, with vasoconstrictive properties. Ropivacaine given epidurally provided…
CAS 38398-32-2
Ganaxolone, also known as CCD 1042 and C1042, is a CNS-selective GABAA modulator that acts on well-characterized targets in the brain known to have anxiolytic and anticonvulsant effects. Ganaxolone protects against seizures in diverse animal models, including…
CAS 360791-49-7
Potent Allosteric Agonist-Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptors
CAS 1793080-72-4
VX-150 is an orally active, highly selective NaV1.8 inhibitor. VX-150 has the potential for various pain indications research[1].
CAS 853400-76-7
Trofinetide, a synthetic analogue of the endogenous N-terminus tripeptide, Glycine-Proline-Glutamate (GPE), has been shown to be neuroprotective in animal models of brain injury.
CAS 516-54-1
Allopregnanolone is a progesterone metabolite. Allopregnanolone is an allosteric modulator of the GABA receptor.
CAS 1072018-68-8
T-Type calcium channel inhibitor is a potent inhibitor of T-Type calcium channel. T-Type calcium channel inhibitor penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished…
CAS 1026029-18-4
AS105 (AS-105) is a highly potent, ATP-competitive CaMKII inhibitor, inhibits CaMKIIδ with IC50 of 8 nM, Ki of 3 nM. AS105 is also effective against autophosphorylated CaMKII (in contrast to the commonly used allosteric CaMKII-inhibitor KN-93). In isolated…
KM822 is avselective, noncompetitive modulator of human dopamine transporter (DAT) with IC50 3.7 μM, which shows 30 and 50 folds higher than for human norepinephrine transporter (hNET) and human serotonin transporter (SERT), respectively.
CAS 129722-12-9
Aripiprazole(Abilify) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.Aripiprazole is an atypical antipsychotic medication used for the treatment of schizophrenia. It has also recently received FDA approval for the treatment of acute manic and…
CAS 71675-85-9
Amisulpride is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder. In Italy, it is also used as a treatment for dysthymia. It was introduced by Sanofi-Aventis in the 1990s. Its patent had expired by…
CAS 2765256-12-8
Novel selective inhibitor of the transient receptor potential melastatin 2 (TRPM2) channel, exhibiting TRPM2 selectivity over TRPM8 and TRPV1 channels as well as phospholipase A2 and showing neuroprotective activity in vitro, and significantly reducing ce
CAS 312753-06-3
Indacaterol is a potent, orally administered ultra-long-acting β2 adrenergic receptor (ADRB2) agonist, widely recognized for its therapeutic potential in respiratory and cardiovascular conditions. By selectively activating ADRB2, indacaterol not only enhances…
CAS 156727-74-1
SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive,…
CAS 80714-61-0
Semax is a synthetic peptide analog of adrenocorticotropic hormone (ACTH) (4-10) that has neuroprotective, analgesic, and anxiolytic properties.In vivo, semax (0.3 mg/kg) reduces cortical nitric oxide (NO) production and the number of neurological…
CAS 616202-92-7
LLorcaserin (APD-356)is a weight-loss drug developed by Arena Pharmaceuticals. It has serotonergic properties and acts as an anorectic
CAS 1146963-51-0
J-147 is a broad spectrum neuroprotective phenyl hydrazide compound(EC50=60-115 nM) with significant neurotrophic properties related to the induction of brain-derived neurotrophic factor (BDNF).IC50 value: 60-115 nM in vitro assay [1]Target: J-147 has been…
CAS 849459-86-5
AC-263093 (AC263093) is a potent, functionally selective neuropeptide FF receptor type 2 (NPFFR2) agonist with pKi of 6.9; shows equal affinity for NPFFR1 and NPFFR2, and functionally inactivated NPFFR1; attenuates morphine tolerance in vivo.
CAS 1331745-61-9
ML372 is a small molecule SMN modulator that increases SMN protein in patient fibroblasts with EC50 of 37 nM; possesses good potency, pharmacokinetics, tolerance, and CNS penetration that are able to increase levels of SMN protein in several model cell lines;…
CAS 202825-46-5
Safinamide mesylate mesylate (FCE 26743 mesylate; EMD 1195686 mesylate) is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide mesylate also blocks sodium channels and modulates…
CAS 854107-55-4
Ponesimod(ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator.
CAS 1744-22-5
Riluzole is an anticonvulsant drug and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
CAS 97-77-8
Disulfiram is a specific inhibitor of?aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol.
CAS 6323-99-5
DL-AP4 (2-Amino-4-phosphonobutyric acid) is a glutamate antagonist. DL-AP4 behaves as a competitive inhibitor of glutamate binding with an apparent Kd of 66 μM. DL-AP4 can be used for the research of central nervous system and visual system[1][2][3].
CAS 153439-40-8
Fexofenadine is a third-generation antihistamine pharmaceutical drug used in the treatment of allergy symptoms, such as hay fever, nasal congestion, and urticaria.
CAS 946387-07-1
RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50values for all three species (hTRPV4: IC50 = 2.3 μM, mTRPV4: IC50 = 5.9 μM, rTRPV4: IC50 = 3.2 μM).IC50 value:…
CAS 409351-28-6
VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ± 93 nM.
CAS 1223405-08-0
Larotrectinib (LOXO-101) sulfate is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
CAS 1821484-84-7
TrkA-IN-23 is a highly potent, subtype selective, peripherally restricted, allosteric TrkA inhibitor with IC50 of 10 nM, 180-fold selective over TrkB and 70-fold selective over TrkC in cell based assays; exhibits exquisite TrkA selectivity with >95%…
CAS 1237541-73-9
NAB-14 is a potent, selective negative allosteric modulator of GluN2C/2D-containing NMDA receptors with IC50 of 580 nM, >800-fold selective over GluN2A/GluN2 receptors; inhibits triheteromeric (GluN1/GluN2A/GluN2C) NMDARs with modestly reduced potency and…
CAS 30123-17-2
Tianeptine sodium salt is a selective facilitator of 5-HT uptake in vitro and in vivo.Tianeptine has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50 > 10 μM) and has no effect on noradrenalin or dopamine uptake. Antidepressant,…
CAS 300803-69-4
A small-molecule inhibitor of STOML3 oligomerization that reverses pathological mechanical hypersensitivity in vivo; effectively inhibits the self-association of stomatin, STOML1 and STOML2 at 2 uM, but not podocin; reversibly reduces the sensitivity of…
CAS 357-08-4
Naloxone is an opioid inverse agonist drug used to counter the effects of opiate overdose.
