Buspirone hydrochloride is an anxiolytic psychotropic drug, is used to treat generalized anxiety disorder (GAD).
Zolmitriptan-d6 is deuterium labeled Zolmitriptan. Zolmitriptan (BW-311C90; 311C90) is a 5-HT1B/1D receptor partial agonist with Kis of 5.01 nM, 0.63 nM, and 63.09 nM for 5-HT1B, 5-HT1D, 5-HT1F receptor, respectively. Zolmitriptan can be used for the research of migraine[1][2].
Sarpogrelate(MCI-9042) hydrochloride, a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD.Target: 5-HT2 RecepterSarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39 nM [1]. Sarpogrelate lacked prominent 5-HT1-like, 5-HT3, beta, H1, H2 and M3 antagonist activity and weakly blocked alpha 1-adrenoceptors (pKB = 6.30). (S)-M-1 showed weak affinity for 5-HT1-like receptors (pKB = 6.30), alpha 1- (pKB = 6.80) and beta- (pKB = 6.54) adrenoceptors, while (R)-M-1 was a weak antagonist at histamine H1 receptors (pKB = 6.49) [2]. After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 +/- 1.7 to 18.1 +/- 2.2 mL/min per 100 mL tissue (P < 0.01) and from 8.2 +/- 0.9 to 14.2 +/- 2.1 mL/min per 100 mL tissue (P < 0.05), respectively. Sarpogrelate-induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. Long-term oral administration of sarpogrelate improves vascular function in patients with PAD [3].
L-Cysteine S-sulfate sodium hydrate is a potent N-methyl-d-aspartate (NMDA) glutamatergic receptors agonist. L-Cysteine S-sulfate sodium hydrate is the substrate for cystine lyase, it can be used in mass spectrometry operations[1][2].
OG-L002 is a potent and highly selective LSD1 inhibitor with an IC50 of 0.02 μM. OG-L002 is a potent monoamine oxidases (MAO) inhibitor with IC50s of 1.38 μM and 0.72 μM for MAO-A and MAO-B, respectively. OG-L002 potently inhibits the expression of HSV IEgenes[1].
NK-1 Antagonist 1 is an antagonist of NK-1 receptor, used in the research of NK-1 related diseases and conditions such as cough, overactive bladder, alcohol dependency and depression.
Mivacurium dichloride is a benzylisoquinoline derivative and is a short-acting non-depolarizing neuromuscular blocking agent and skeletal muscle relaxant. Mivacurium dichloride couples with the nAChR to reduce or inhibit the depolarizing effect of acetylcholine on the terminal disc of the muscle cell[1][2][3].
Mulberrofuran H is a 2-arylbenzofuran derivative from the cultivated mulberry tree (Morus lhou (ser.) Koidz.). Mulberrofuran H demonstrates potent inhibition against substrates L-tyrosine (IC50=4.45 µM) and L-DOPA (IC50=19.70 µM). Mulberrofuran H also shows potent anti-inflammatory and antioxidative activities[1][2][3].
Acremonidin A is a potent calmodulin (CaM) inhibitor found in Purpureocillium lilacinum. Acremonidin A binds to the human calmodulin (hCaM) biosensor hCaM M124C-mBBr, with Kd of 19.40 nM[1].
Dehydrodiscretamine chloride is a dual inhibitor of AChE and BChE with IC50s of 17.8 and 118.8 μM, respectively. Dehydrodiscretamine chloride has antioxidant activity. Dehydrodiscretamine chloride can be used in study Alzheimer’s disease[1].
Biperiden(KL 373) is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker.Target: M1 receptorsBiperiden is an antiparkinsonian agent of the anticholinergic type. It is used for the adjunctive treatment of all forms of Parkinson's disease (postencephalitic, idiopathic, and arteriosclerotic)[1]. Biperiden has an atropine-like blocking effect on all peripheral structures which are parasympathetic-innervate. It also has a prominent central blocking effect on M1 receptors [2].Biperiden (0.11 mg/kg), benactyzine (0.3 mg/kg),caramiphen (10 mg/kg), procyclidine (3 mg/kg), and trihexyphenidyl (0.12 mg/kg) separately and each in combination with physostigmine (0.1 mg/kg) is to make a comparative assessment of potential cognitive effects. The results showed that benactyzine, caramiphen, and trihexyphenidyl reduced rats' innate preference for novelty, whereas biperiden and procyclidine did not [3].Clinical indications: parkinsonismFDA Approved Date: Toxicity: Drowsiness; vertigo; headache; dizziness
Ferulamide is a Ferulic acid derivative isolated from Portulaca oleracea L. with anticholinesterase activities[1][2].
Mecamylamine is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine is also a ganglionic blocker. Mecamylamine can across the blood-brain barrier. Mecamylamine can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area[1][2][5].
β-Amyloid (31-35) is the shortest sequence of native Amyloid-β peptide that retains neurotoxic activity.
LY 278584 is a potent, highly selective 5-HT3 receptor antagonist with a Ki of 1.62 nM. LY 278584 has no activity on 5-HT1A, 5-HT1B, 5-HT1C, 5-HT1D, or 5-HT2 receptors[1].
Ondansetron-d3 is the deuterium labeled Ondansetron[1]. Ondansetron(GR 38032;SN 307) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy[2].
Decanoic acid-d5 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
LY3202626 is a small molecule non-selective BACE1 inhibitor, causes dose-dependent reductions in CSF and plasma Aβ concentrations, shows potential for the treatment of Alzheimer's disease. Alzheimer Disease Phase 2 Clinical
Tedatioxetine hydrobromide acts as a triple reuptake inhibitor and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist.
[Tyr22] Calcitonin Gene Related Peptide, (22-37), rat is a fragments 22-37 of rat calcitonin gene related peptide (CGRP), targeting CGRP receptor and adenylate cyclase. Calcitonin is mainly produced by thyroid C cells while CGRP is secreted and stored in the nervous system[1].
β-casomorphin, bovine (β-casomorphin-7) is a opioid peptide with an IC50 of 14 μM in an Opioid receptors binding assay.
Afacifenacin (SMP-986) is a potent and orally active muscarinic receptor antagonist. Afacifenacin inhibits the bladder afferent pathway through the sodium-channel blockade, increasing volume, and reducing the frequency of urination and incontinence. Afacifenacin has the potential for the research of overactive bladder (OAB)[1][2].
(-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site[1].
Remimazolam (CNS-7056) is a short-acting GABA(A) receptor agonist[1].
Inaperisone is a centrally acting muscle relaxant. Inaperisone inhibits the micturition reflex by acting indirectly on GABAB receptors in the brainstem[1].
PPPA is a competitive NMDA receptor antagonist that displays moderate selectivity for NR2A-containing receptors[1][2].
trans-ACBD (trans-1-Aminocyclobutane-1,3-dicarboxylic acid) is a very potent and selective NMDA receptor agonist that modulates glutamatergic neurotransmission[1].
Glycerophosphoinositol choline is an essential nutrient that activates alpha7 nicotinic receptors and has analgesic and anti-inflammatory activity. Glycerophosphoinositol choline can affect diseases such as liver disease, atherosclerosis and neurological disorders[1][2].
Cisapride monohydrate is an orally and potent 5-HT4 receptor agonist and hERG inhibitor. Cisapride monohydrate is an prokinetic agent which facilitates or restores motility throughout the length of the gastrointestinal tract. Cisapride monohydrate stimulates gastrointestinal motor activity through an indirect mechanism involving the release of acetylcholine mediated by postganglionic nerve endings in the myenteric plexus of the gut[1][2].
AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research[1].