SB-366791 is a potent , competitive and selective vanilloid receptor (VR1/TRPV1) antagonist with IC50 of 5.7±1.2 nMtarget: VR1/TRPV1IC 50: 5.7±1.2 nM [1] SB-366791 produced a concentration-dependent inhibition of the response to capsaicin with an apparent pKb of 7.74±0.08. Schild analysis indicated a competitive mechanism of action with a pA2 of 7.71.[1] SB-366791 showed a concentration-dependent potentiation of pH 5-induced 45Ca2+uptake in CHO cells expressing rat TRPV1 but not in untransfected cells[2]
Lupanin (D-Lupanine) is a natural ketonic derivative of Sparteine ((+)-Sparteine (HY-W008350)) with a ganglioplegic activity. Lupanine shows binding affinity for nicotinic receptor (nAChR) with a Ki value of 500 nM[1].
3,5-Dihydroxy-2-naphthoic acid is a Naphthoic acid derivative. Naphthoic acid is a NMDA receptor allosteric modulator[1].
Lamotrigine-13C,d3 is the 13C- and deuterium labeled. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al[1][2].
Dronedarone D6 hydrochloride is the deuterium labeled Dronedarone. Dronedarone hydrochloride, a derivative of Amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone hydrochloride is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone hydrochloride is a substrate for and a moderate inhibitor of CYP3A4[1][2][3][4].
Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively[1].
HC-067047 is a potent and selective TRPV4 antagonist with IC50s of 48 nM, 133 nM, and 17 nM for human, rat, and mouse TRPV4.
tracurium (BW-33A free acid) is a potent, competitive and non-depolarizing neuromuscular blocking agent.Atracurium also is an AChR receptor antagonist. Atracurium induces bronchoconstriction and neuromuscular blockade. Atracurium promotes astroglial differentiation[1][2][3][4][5].
Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone potassium is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer[1][2][4][7].
BCRP-IN-1 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
Y-27152, a prodrug of the KATP (Kir6) channel opener Y-26763, is a long-acting K+ channel opener with less tachycardia: antihypertensive effects in hypertensive rats and dogs in conscious state[1][2].
GX-674 is a potent, state-dependent, isoform-selective voltage-gated sodium channel 1.7 (Nav1.7) antagonist with an IC50 of 0.1 nM at -40 mV[1].
Bumetanide D5 is a deuterium labeled Bumetanide. Bumetanide is a selective Na+-K+-Cl- (NKCC1) inhibitor, weakly inhibits NKCC2, with IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively[1].
N-Salicyloyltryptamine acts on voltage-dependent Na+, Ca2+, and K+ ion channels inhibitor. N-Salicyloyltryptamine inhibits K+ currents with an IC50 value of 34.6 μM (Ito). N-Salicyloyltryptamine also exhibits anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect[1]-[5].
JNc-440 is a small molecule that significantly and specifically strengthens the TRPV4-KCa2.3 interaction in mouse endothelial cells, but does not systemically activate TRPV4 and KCa2.3; shows affinity for both TRPV4 and KCa2.3, enhances vasodilation and exerts antihypertensive effects in mice.
Rilmazafone is a benzodiazepine (omega) ligand with sedative and hypnotic effects[1].
Piperidine-4-sulfonic acid is a potent GABA agonist with an IC50 of 0.034 μM for the inhibition of the binding of H-GABA[1].
Dantrolene sodium is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ from the sarcoplasm. Dantrolene sodium is a skeletal muscle relaxant which acts by blocking muscle contraction beyond the neuromuscular junction.
Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca2+ influx and Ca2+ cell overload[1][2][3].
Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
Dyclonine is an oral anaesthetic found in Sucrets, an over the counter throat lozenge.Target: Sodium ChannelDyclonine is an oral anaesthetic that is the active ingredient of Sucrets, an over the counter throat lozenge. It is also found in some varieties of the Cepacol sore throat spray. It is a local anesthetic, used topically as the hydrochloride salt. Dyclonine hydrochloride has been found to possess, in addition to its topical anesthetic properties, significant bactericidal and fungicidal activity. Self-sterilizing action manifested by preparations containing the drug was considerably enhanced upon the addition of chlorobutanol. Results of in vitro tests employing microorganisms commonly involved in local infections indicated that the two agents in combination act synergistically [1, 2].
Gomisin J is a small molecular weight lignan found in Schisandra chinensis and has been demonstrated to have vasodilatory activity[1]. Gomisin J suppresses lipid accumulation by regulating the expression of lipogenic and lipolytic enzymes and inflammatory molecules through activation of AMPK, LKB1 and Ca2+/calmodulin-dependent protein kinase II and inhibition of fetuin-A in HepG2 cells. gomisin J has potential benefits in treating nonalcoholic fatty liver disease[2].
Norfluoxetine hydrochloride is an active N-demethylated metabolite of Fluoxetine. Fluoxetine is a selective serotonin (5-HT) reuptake inhibitor that is metabolized to Norfluoxetine hydrochloride by cytochrome P450 (CYP) 2D6, CYP2C19, and CYP3A4. Norfluoxetine hydrochloride inhibits 5-HT uptake and inhibits CaV3.3 T current (IC50 = 5 μM). Norfluoxetine hydrochloride has anticonvulsant activity[1][2][3][4].
Phrixotoxin 2 is a highly selective KV4.2 and KV4.3-channels blocker[1].
Talampanel is a potent and selective AMPA-receptor antagonist, is a potential new antiepileptic drug (AED). Target: AMPA [1]in vitro: Talampanel is a glutamate receptor inhibitor with anti-seizure activity.in vivo： Talampanel reduces motoneuronal calcium in a mouse model of ALS, but its effi cacy declines as the disease progresses, suggesting that medication initiation in the earlier stages of the disease might be more effective. [2]
MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The Kis are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC50s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity[1].
Linopirdine (DUP-996) is a potent Kv7 (KCNQ) voltage-gated potassium channels blcoker; blocks KV7.1+7.3 (KCNQ2+3) / M-currents (IC50=4-7 uM) and KV7.1 (KCNQ1) homomeric channels (IC50=8.9 uM); inhibits M-type K+ current, increases acetylcholine release in rat hippocampal CA1 neurons; active in vivo. Alzheimer Disease Phase 1 Discontinued
UB-165 is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for [3H]-nicotine binding in rat brain[1].
(S)-Cipepofol is the inactive isomer of Cipepofol (HY-116152).Cipepofol (HSK3486) is a sleep-promoting active molecule and a gamma-aminobutyric acid (GABA) receptor enhancer[1].
PEAQX(NVP-AAM 077) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B(29,600 nM).IC50 value: 270 nM(hNMDA A1/A2) [1]Target: NR2A antagonistin vitro: PEAQX has a high binding affinity for NMDA receptors (IC50=8 nM), and a functional preference in excess of 100-fold for hNMDA 1A/2A (IC50=of 270 nM) over 1A/2B receptors (IC50=29,600 nM) [1].in vivo: PEAQX is practically inactive in Xenopus oocytes expressing hNMDA 1A/2B receptors, displays an ED50 value of 23 mg/kg in the MES test [1]. Sprague-Dawley rats were treated on PN7, PN9, and PN11 with PCP (10 mg/kg), PEAQX (NR2A-preferring antagonist; 10, 20, or 40 mg/kg), or ifenprodil (selective NR2B antagonist; 1, 5, or 10 mg/kg) and sacrificed for measurement of caspase-3 activity (an index of apoptosis) or allowed to age and tested for locomotor sensitization to PCP challenge on PN28-PN35. PCP or PEAQX on PN7, PN9, and PN11 markedly elevated caspase-3 activity in the cortex; ifenprodil showed no effect. Striatal apoptosis was evident only after subchronic treatment with a high dose of PEAQX (20 mg/kg). Animals treated with PCP or PEAQX on PN7, PN9, and PN11 showed a sensitized locomotor response to PCP challenge on PN28-PN35 [2].