α-Conotoxin TxID is a potent α3β4 nAChR antagonist with an IC50 value of 12.5 nM. α-Conotoxin TxID has weak inhibition activity of closely related α6/α3β4 nAChR (IC50= 94 nM). α-Conotoxin TxID has the potential for novel smoking cessation drug development[1].
AA29504 is a ethyl carbamate with γ-aminobutyric acid (GABAA(HY-L120) receptor activity. AA29504 inhibits the delivery of the neurotransmitter gamma-aminobutyric acid in the central nervous system. AA29504 can be used to research anxiety, insomnia and other neuropsychiatric diseases [1].
Quifenadine (Compound 3a), the hydroxyl-(diphenyl)methyl quinuclidine derivative, is a M3 receptor antagonist with an IC50 value > 1000 nM. Quifenadine can be used for the research of neurological disease[1].
Phenylbiguanide is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM.
Vanicoside E is an antioxidant and antitumor agent. Vanicoside E inhibits L-Tyrosine (HY-N0473) and L-DOPA (HY-N0304) with IC50s of 45.23 μM and 189.96 μM, respectively[1][2].
Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist.The reference for administration is 10 mg/kg.
Opiranserin (VVZ-149, VVZ-000149) is a potent, selective, mixed glycine GlyT2 transporter blocker (IC50= 0.86 uM), purine P2X3 receptor antagonist (IC50=0.87 uM) and serotonin 5-HT2A receptor antagonist (IC50=1.3 uM); demonstrates analgesic efficacy for postoperative pain. Pain Phase 2 Clinical
Cassiaside is a naphthopyrone glucoside, shows mixed-type inhibition against BACE1 (IC50=4.45 μM; Ki=9.85 μM). Cassiaside possesses potential anti- Alzheimer's disease (AD) activity[1].
DALDA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA shows antinociceptive and respiratory effects[1].
RS 8359 is a selective and reversible MAO-A inhibitor, with antidepressant activity.
VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. VU 6008667 has high CNS penetration[1].
Oxyphencyclimine is an orally active muscarinic receptor (mAChR) antagonist. Oxyphencyclimine is effective in reducing ulceration index and increasing pepsin activity in rat gastric ulcer model. Oxyphencyclimine can be used in studies of peptic ulcer disease and gastrointestinal spasm[1][2].
Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs)[1][2][3][4].
PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively, and is inactive for other muscarinic receptors. PQCA improves cognitive performance and cerebral blood flow in rat, cynomolgus macaque, and rhesus macaque. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease[1][2].
LY2886721 is an BACE inhibitor used for the treatment of Alzheimer's Disease.IC50 value:Target: BACELY2886721 is a novel potent agent that is used to treat Alzheimer’s Disease in preclinical experiments. LY2886721 is under clinical study. A Safety Study of LY2886721 Multiple Doses is performing in Healthy Subjects.
Zuclopenthixol-d4((Z)-Clopenthixol-d4) succinate salt is the deuterium labeled Zuclopenthixol. Zuclopenthixol is a thioxanthene derivative which acts as a mixed dopamine D1/D2 receptor antagonist[1][2].
Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist. Pridopidine exerts high affinity towards sigma 1 receptor (S1R) with Ki between 70 and 80 nM, which is ~100× higher than its affinity toward D2R.
ABT-702 dihydrochloride is a potent adenosine kinase (AK) inhibitor (IC50=1.7 nM).
Gallamine Triethiodide is a synthetic nondepolarizing blocking drug.Target: mAChRGallamine triethiodide is a non-depolarising muscle relaxant. It acts by combining with the cholinergic receptor sites in muscle and competitively blocking the transmitter action of acetylcholine. Gallamine triethiodide has a parasympatholytic effect on the cardiac vagus nerve which causes tachycardia and occasionally hypertension. Very high doses cause histamine release. Gallamine triethiodide is commonly used to stabilize muscle contractions during surgical procedures. From Wikipedia.
Clomipramine HCl is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively. Target: 5-HT ReceptorClomipramine hydrochloride (Anafranil) is a hydrochloride salt of clomipramine which is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively. Clomipramine hydrochloride (Anafranil) is a tricyclic antidepressant. Clomipramine hydrochloride (Anafranil) is a norepinephrine-reuptake inhibitor and is an antiobsessional drug. Clomipramine hydrochloride (Anafranil) is an antagonist/inverse agonist at the following receptors: D2 receptor (Ki = 162 nM), D3 receptor (Ki = 30 nM), α1-adrenergic receptor (Ki = 3.2 nM), α2-adrenergic receptor (Ki = 525 nM), H1 receptor (Ki = 31 nM), mACh receptors (Ki = 37 nM), 5-HT2A receptor (Ki = 36 nM), 5-HT2C receptor (Ki = 65 nM), 5-HT3 receptor (Ki = 85 nM), 5-HT6 receptor (Ki = 54 nM), 5-HT7 receptor (Ki = 127 nM), D1 receptor (Ki = 219 nM) [1-3].
Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC)[1].
NNC05-2090 (hydrochloride) is a GABA uptake inhibitor. NNC05-2090 is a betaine/GABA transporter (BGT-1) inhibitor with an IC50 value of 10.6 μM. NNC05-2090 can be used for the research of epilepsy and neurological disease[1][2].
RPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE[1].
Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin.
Drofenine hydrochloride is a potent competitive inhibitor of BChE, and the ki values of Drofenine is calculated to be 3 uM.IC50 value: 3 uM (ki)Target: BChEBenactyzine is widely used anticholinergic drugs, acts on smooth muscle to stop muscle spasms.
Galanthamine N-Oxide is an alkaloid obtained from the bulbs of Zephyranthes concolor. Galanthamine N-Oxide inhibits electric eel acetylcholinesterase (AChE) with an EC50 of 26.2 μM. Galanthamine N-Oxide is a prominent inhibitor of substrate accommodation in the active site of the Torpedo californica AChE (TcAChE), hAChE and hBChE enzymes[1][2].
Duloxetine-d7 ((S)-Duloxetine-d7) is the deuterium labeled Duloxetine. Duloxetine is a serotonin-norepinephrine reuptake inhibitor with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD)[1][2].
7-Hydroxy-3,4-dihydro-2(1H)-quinolinone is a weak MAO-A inhibitor, with an IC50 of 183 μM, and has no effect on MAO-B[1].
Jujuboside A is a glycoside extracted from Semen Ziziphi Spinosae, a Chinese herbal medicine used to treat insomnia and anxiety.
Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC500s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.