BIO-acetoxime (BIA) is a potent and selective GSK-3 inhibitor, with IC50s of both 10 nM for GSK-3α/β. BIO-acetoxime has anticonvulsant and anti-infection activity.
GMQ is a ASIC (acid-sensing ion) channel activator with an EC50 value of 1.83 mM for ASIC3 at pH 7.4. GMQ opens only ASIC3 but no other ASICs at pH 7.4. GMQ can be used for neurological disease research[1].
DL-Gabaculine hydrochloride is a neurotoxin that irreversibly inhibits bacterial pyridoxal phosphate linked γ-aminobutyric acid-α-ketoglutaric acid transaminase with a Ki of 2.86 μM[1].
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors[1].
Heteropodatoxin-2, a peptides of 30-amino acid, is a heteropodatoxin. Heteropodatoxin-2 blocks Kv4.2 current expressed in Xenopus laevis oocytes in a voltage-dependent manner, with less block at more positive potentials[1].
Alarin (human) is a hypothalamic neuropeptide belonging to the galanin family of peptides. Alarin (human) has the signal sequence of the GALP precursor peptide and the first 5 aa of the mature GALP[1].
GPI-1485 (GM1485), a nonimmunosuppressive immunophilin ligand, promotes neurofunctional improvement and neural regeneration following stroke[1].
Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects[1][2].
Oxcarbazepine inhibits the binding of [3H]BTX to sodium channels with IC50 of 160 μM and also inhibits the influx of 22Na+ into rat brain synaptosomes with IC50 about 100 μM.Target: Sodium ChannelOxcarbazepine is an antiepileptic drug with a chemical structure similar to carbamazepine, but with different metabolism. Oxcarbazepine is rapidly reduced to 10,11-dihydro-10-hydroxy-carbazepine (monohydroxy derivative, MHD), the clinically relevant metabolite of oxcarbazepine. MHD has (S)-(+)- and the (R)-(-)-enantiomer [1]. Oxcarbazepine (oxcarb) 600 and 900 mg (2360 and 3540 mumol) was taken by 3 volunteers (2 female, 1 male; 45-67 kg; age 22-34 years) after an overnight fast. Blood, saliva and urine were collected for the next 72 h for assay of oxcarb, 10,11-dihydro-10-hydroxy-carbamazepine (OHcarb), and 10,11-dihydro-trans-10,11-dihydroxy-carbamazepine (diol). Oxcarb reached a maximum level of about 1 microgram/ml (3.93 mumol/l) within 1 h and dropped below the detection limit (0.1 microgram/ml = 0.39 mumol/l) within 3 h. The active metabolite OHcarb appeared in the blood before oxcarb and reached the higher maximum level of 7.4 microgram/ml (29 mumol/l) after 7 h [2]. Clinical indications: EpilepsyToxicity: Isolated cases of overdose with oxcarbazepine have been reported. The maximum dose taken was approximately 24,000 mg. All patients recovered with symptomatic treatment.
Cevostamab (BFCR4350A; RG6160; RO7187797) is a humanized IgG1-based BsAb that targets membrane-proximal extracellular domain of FcRH5 on multiple myeloma (MM) cells as well as CD3 on T cells. Moreover, Cevostamab facilitates efficient synapse formation, improves killing activity of T cells against MM tumor cells[1][2].
UBP-282 is a potent, selective and competitive AMPA and kainate receptor antagonist. UBP-282 inhibits the fast component of the dorsal root-evoked ventral root potential (fDR-VRP) with an IC50 value of 10.3 μM. UBP-282 antagonizes kainate-induced depolarisations of dorsal roots with a pA2 value of 4.96[1][2].
LE 300 is a potent and selective dopamine D1-like receptor antagonist with Kis of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT2A receptor with a pA2 of 8.32 in a rat tail artery assay[1][2].
D-erythro-MAPP (D-e-MAPP) is a ceramidase inhibitor, with an IC50 of 1-5 μM in vitro[1].
PF-03049423 (Compound PF-5) free base is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of about 0.2 nM for rat and human platelet enzyme. PF-03049423 free base can be used for the research of acute ischaemic stroke[1].
NP-1815-PX sodium is a potent and selective P2X4R antagonist. NP-1815-PX sodium has anti-inflammatory activity, and can relieve pain in chronic pain models. NP-1815-PX sodium also inhibits guinea pig tracheal/bronchial smooth muscle (TSM and BSM) contractions[1][2][3].
(-)Clausenamide is an active alkaloid isolated from the leaves of Clausena lansium (Lour.) Skeels, and improves cognitive function in both normal physiological and pathological conditions. (-)Clausenamide inhibits β-amyloid (Aβ) toxicity, blocking neurofibrillary tangle formation by inhibiting the phosphorylation of tau protein.
Aposcopolamine is an alkaloid that can be isolated from Datura ferox. Aposcopolamin can closely binds with ACHE, ADRA2A and CHRM2. Aposcopolamine can be used for the research of Alzheimer's disease[1].
α-Conotoxin SIA is a selective nicotinic acetylcholine receptor (nAChR) antagonist with high affinity for the muscle nAChR. α-Conotoxin SIA preferentially targets the α/δ interface of the muscle nAChR in mouse muscle. In contrast, for Torpedo nAChR, α-Conotoxin SIA has a much higher affinity for the α/γ than for the α/δ interface[1].
Kissoone C (compound 3) is a three-membered ring sesquiterpene isolated from valerian root. Kissoone C can enhance the activity of nerve growth factor (NGF)-mediated neurite outgrowth in PC12D cells[1].
Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [3H]histamine release. Thioperamide inhibits [3H]histamine synthesis with a Ki of 31 nM[1].
NPT200-11 is a brain penetrating inhibitor of accumulation of alpha-synuclein (ASYN) misfolding and aggregation. NPT200-11 can be used for research of Parkinson's disease[1].
(R)-DRF053 dihydrochloride (DRF053) is a potent, cell-permeable, dual CK1/CDK inhibitor with IC50 of 14 nM, 220 nM and 80 nM for CK1, CDK5/p25 and CDK1/cyclin B, respectively; exhibits antiproliferative activity against human neuroblastoma SH-SY5Y cells with EC50 of 17.2 uM, prevents the CK1-dependent production of amyloid-beta in a cell model; specifically increases the number of duct-derived β-cells without affecting their proliferation.
CL 218872 is a selective and orally active benzodiazepine of α1 subunit-containing GABAAreceptor with a Ki of 130 nM. CL 218872 exerts anxiolytic and anticonvulsant in vivo[1].
SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
Olvanil (NE-19550)is an agonist of transient receptor potential vanilloid type 1 (TRPV1) channels with an EC50 of 0.7 nM.Analgesic[1].
(-)-Securinine is plant-derived alkaloid and also a GABAA receptor antagonist.
Fulranumab is a human IgG2 monoclonal antibody against nerve growth factor (NGF) and can be used for the research of pain[1].
L-745870 is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors affinity. L-745870 has excellent brain penetration[1][2][3].
ABT-724 is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile[1].