Neurotransmission, neural targets and neurological research.
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Other Research Tools (75) · Additional reagents, building blocks and specialized research tools.
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CAS 475205-49-3
A-317491 is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors.It is known that P2X3 and P2X2/3 receptors stimulate the pronociceptive effects of ATP upon activation. Studies indicate that the P2X3…
CAS 123557-91-5
rac-BHFF is a potent and orally active allosteric enhancer of GABAB receptor[1].
CAS 120-97-8
Dichlorphenamide(Diclofenamide) is a carbonic anhydrase inhibitor that is used in the treatment of glaucoma.Dichlorphenamide is a sulfonamide and a carbonic anhydrase inhibitor of the meta-Disulfamoylbenzene class. This drug has the same side-effects as…
CAS 1030377-33-3
Suvorexant (MK-4305) is a potent, selective, and orally bioavailable antagonist of OX1R and OX2R currently under clinical investigation as a novel therapy for insomnia.
CAS 16562-13-3
L-Stepholidine (Stepholidine), an alkaloid extract of the Chinese herb Stephania intermedia, is the first compound known to exhibit mixed dopamine D1 receptor agonist/D2 antagonist properties. L-Stepholidine (Stepholidine) has neuroprotective effect and…
CAS 1984824-54-5
GDC-0334 (GDC0334) is a highly potent, selective, orally bioavailable TRPA1 antagonist with IC50 of 1.7 nM in cell-based assays.GDC-0334 demonstrated potent TRPA1 inhibition in several species, including human (IC50=1.7 nM), cynomolgus (IC50=3.6 nM), mouse…
CAS 6202-23-9
Cyclobenzaprine Hcl is a skeletal muscle relaxant and a central nervous system (CNS) depressant.Cyclobenzaprine is a skeletal muscle relaxant and a central nervous system (CNS) depressant. Cyclobenzaprine was thought to be an alpha 2-adrenoceptor agonist that…
CAS 1235318-89-4
ADX88178 is a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4) with EC50 of 4 nM for human mGluR4.
CAS 147817-50-3
Siramesine(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.lysosome-destabilizing agentsiramesine can induce rapid cell death in a number of…
CAS 659730-32-2
AMG 517 is a potent and selective vanilloid receptor-1 (TRPV1) antagonist with an IC50 of 0.5 nM.
CAS 190786-44-8
Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist.
CAS 1020315-31-4
PF-04457845 is a highly efficacious and selective FAAH inhibitor with IC50 values is 7.2±0.63 nM and 7.4±0.62 nM for hFAAH and rFAAH, respectively.
CAS 1227163-84-9
AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor.
CAS 1333207-63-8
SAR7334 hydrochloride is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.
CAS 1316755-16-4
Olodanrigan (EMA401), a highly selective AT2R antagonist, inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.
CAS 1235560-28-7
ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
CAS 1331782-27-4
PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat…
CAS 192322-50-2
CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes.
CAS 5001-32-1
Guanoclor is a sympatholytic drug. It is known to bind to non-adrenergic sites in pig kidney membranes.
CAS 913830-15-6
NS9283 is a positive positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. NS9283 can be used in a series of neurological conditions such as attention deficit hyperactivity disorder (ADHD), schizophrenia, Parkinson's disease and Alzheimer's…
CAS 1118460-77-7
UCPH-101 is an excitatory amino acid transporter subtype 1 (EAAT1) inhibitor with an IC50 of 0.66 μM.
CAS 865305-30-2
AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0).
CAS 21102-95-4
BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3.
CAS 106516-24-9
Sertindole, a neuroleptic, is one of the newer antipsychotic medications available.In vitro studies showed that sertindole exerts a potent antagonism at serotonin 5-HT2A, 5-HT2C, dopamine D2, and αl adrenergic receptors. Sertindole offers an alternative…
CAS 545380-34-5
QNZ shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. EVP4593 is a neuroprotective inhibitor of SOC channel.
CAS 1373765-19-5
IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
CAS 1402727-29-0
PE859 is a potent inhibitor of both tau and Aβ aggregation with IC50 values of 0.66 and 1.2 μM, respectively.
CAS 1632051-40-1
Zuranolone(SAGE-217, CS-2797) is an orally active and potent neuroactive steroid and positive allosteric modulator of the GABAA receptor, with EC50s of 296 nM for α1β2γ2 receptor.
CAS 607742-69-8
SB742457 is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors.SB-742457, a 5-HT6 receptor antagonist, which extends into Alzheimer disease (AD) sufferers further highlights the therapeutic…
CAS 168273-06-1
Rimonabant(SR141716) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.
CAS 138356-21-5
BD-1047 dihydrobromide is a selective functional antagonist of sigma receptors, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia.
CAS 23651-95-8
Droxidopa(L-DOPS, SM5688) is a synthetic amino acid precursor which acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline); capable of crossing the protective blood–brain barrier.The acute administration of…
CAS 219766-25-3
ANA-12 is a potent and selective TrkB antagonist with IC50s of 45.6 nM and 41.1 μM for the high and low affinity sites, respectively.
CAS 1820812-16-5
TAK-071 is a novel muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM[1].
CAS 1303420-67-8
PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor, for extended and specific microglial elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals[1].
CAS 1141934-97-5
Emixustat hydrochloride strongly inhibits 11-cis-retinol production with IC50 values of 232 ± 3 nM.Emixustat hydrochloride is a novel visual cycle modulator, in healthy volunteers. Oral Emixustat was safe and well tolerated when administered once daily for 14…
CAS 1235403-62-9
PF 05089771 is a Nav1.7 channel blocker extracted from patent WO/2010/079443 A1, compound example 788, has an IC50 of 8.6 nM.
CAS 148642-42-6
GR-127935 potent and selective 5-HT1B/1D receptor antagonist with pKi of 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptor.
CAS 903576-44-3
Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
CAS 161832-65-1
Talampanel is a potent and selective AMPA-receptor antagonist, is a potential new antiepileptic drug (AED).
CAS 545395-94-6
AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.
CAS 1005334-57-5
CVT-10216 is a highly selective, reversible aldehyde dehydrogenase-2 (ALDH-2) inhibitor with an IC50 of 29 nM. CVT-10216 also has inhibitory effect of ALDH-1 with an IC50 of 1.3 μM. CVT-10216 can reduces excessive alcohol drinking in alcohol-preferring rats…
CAS 864821-90-9
Eluxadoline is an orally active mixed μ opioid receptor (μOR) agonist δ opioid receptor (δOR) antagonist. in vitro: Eluxadoline is a locally active, mixed ?-opioid receptor (?OR) agonist and δ-opioid receptor (δOR) antagonist being developed for the treatment…
CAS 328232-95-7
MK-0557 is a highly selective, orally available neuropeptide Y5 receptor antagonist with a Ki of 1.6 nM.
CAS 116209-55-3
Levobetaxolol hydrochloride is a beta-adrenergic receptor inhibitor (beta blocker), used to lower the pressure in the eye in treating conditions such as glaucoma.
CAS 6104-71-8
N-Desmethylclozapine is a dengue virus inhibitor, and an agonist of δ-opioid receptor.
