(R)-SKF 38393 ((±)-SKF-38393) hydrochloride is a potent and selective D1 dopamine receptor antagonist. (R)-SKF 38393 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channel[1].
PF-05150122 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5. Pain Phase 1 Discontinued
CaV1.3 antagonist-1 is a potent and highly selective CaV1.3 L-type calcium channel (LTCC) antagonist with an IC50 of 1.7 μM. CaV1.3 antagonist-1 inhibits CaV1.3 LTCC >600-fold more potently than CaV1.2 LTCC. CaV1.3 antagonist-1, a cyclopentyl derivative, has the potential for Parkinson's disease research[1].
N-Desethyl Oxybutynin D5 hydrochloride is deuterium labeled N-Desethyl Oxybutynin hydrochloride. N-Desethyl Oxybutynin is the the active metabolite Oxybutynin. Oxybutynin is an anticholinergic agent that inhibits voltage-dependent K+ channels[1].
AChE/BChE-IN-8 (Compound 5a) is an uncompetitive AChE and mixed BChE inhibitor with Ki values of 0.788 μM and 2.364 μM against Electrophorus electricus AChE (EeAChE) and equine BChE (eqBChE), respectively. AChE/BChE-IN-8 can cross the BBB and has low cytotoxicity[1].
HDAC1/MAO-B-IN-1 is a potent, selective and cross the blood-brain barrier HDAC1/MAO-B inhibitor with IC50 values of 21.4 nM and 99.0 nM for HDAC1 and MAO-B, respectively. HDAC1/MAO-B-IN-1 has the potential for the research of Alzheimer’s disease[1].
LPLRF-NH2 is a member of RFamide peptide with anorexigenic effect. LPLRF-NH2 increases arterial blood pressure and modulates the electrical activity of brainstem neurons[1][2][3].
Isoimperatorin is a methanolic extract of the roots of Angelica dahurica shows significant inhibitory effects on acetylcholinesterase (AChE) with the IC50 of 74.6 μM.
Flaconitine is isolated from the ammonium hydroxide wetted root of A.szechenyianum Gay. Flaconitine is considered to be a NF-κB inhibitor.
Azasetron HCl is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy. Target: 5-HT3 ReceptorAzasetron Hydrochloride is a 5-HT3 receptor antagonist which is used as an anti-emetic.Azasetron inhibited the specific binding of [3H]quipazine to 5-HT3 receptors at the synaptic membranes of the rat cerebral cortex with a Ki value of 2.9 nM. Azasetron showed low affinity for histamine H1 receptors (IC50 = 4.4 microM) but it could not reveal any affinities for the other receptors (5-HT1A, 5-HT2, dopamine D1, dopamine D2, alpha 1-adrenoceptor, alpha 2-adrenoceptor, muscarine and benzodiazepine) even at a 10 microM concentration [1]. Azasetron (0.1-1.0 mg/kg) dose-dependently prolonged the latency to the first vomiting and decreased the number of vomitings induced by cisplatin in dogs. Azasetron is an orally active antiemetic compound against cisplatin and doxorubicin/cyclophosphamide-induced emeses; and its the antiemetic potency is similar to those of granisetron and ondansetron, but superior to those of metoclopramide and domperidone [2].
Agouti-Related Protein (54-82) (human) (AGRP (54-82) (human)) is an amino-terminal 54-82 fragment of agouti-related protein (AGRP)[1].
Hypotaurine (2-aminoethanesulfinic acid), an intermediate in taurine biosynthesis from cysteine in astrocytes, is an endogenous inhibitory amino acid of the glycine receptor.
c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-Agm is a is a potent, selective and short-acting peptidic V2 receptor (V2R) agonist with EC50s of 0.25 and 0.05 nM for hV2R and rV2R, respectively[1].
Tamsulosin hydrochloride((R)-(-)-YM12617;LY253351) is a selective α1 receptor antagonist.Target: α1 receptorTamsulosin is a selective α1 receptor antagonist that has preferential selectivity for the α1A receptor in the prostate versus the α1B receptor in the blood vessels. Tamsulosin-treated patients had a 0.30-fold lower risk of developing acute urinary retention compared with control patients. None of the International Continence Society male questionnaire domain scores showed significant changes between the groups [1]. tamsulosin can be recommended for treating men after catheterization for AUR, and can reduce the likelihood of the need for re-catheterization [2].
FGFR-IN-3 (compound 6) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-3 shows neuroprotective activity. FGFR-IN-3 can be used for neurodegenerative diseases research[1].
Clathrin-IN-4 (compound 8b), a Wiskostatin (HY-12534) analogue, is a potent inhibitor of clathrin mediated endocytosis with an IC50 of 2.1 μM. Clathrin-IN-4 is a dynamin I GTPase activity inhibitor with an IC50 of 9.1 μM[1].
GIBH-130 is an effective inhibitor of neuroinflammation. GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50=3.4 nM).
Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research[1][2].
VU0366248 is a mGlu5 negative allosteric modulator[1].
Bethanechol is a parasympathomimetic choline carbamate that selectively stimulates muscarinic receptors without any effect on nicotinic receptors.Target: muscarinic receptorHyoscine butylbromide concentration dependently reduced muscle contractions, calcium mobilization, and epithelial secretion induced by the muscarinic agonist bethanechol with IC50 values of 429, 121, and 224 nmol L(-1), respectively.[2] Bethanechol presentes significantly improve of salivary parameters. Bethanechol is effective in decreasing the salivary gland damage.[3] Cerebral malakoplakia is a very rare chronic inflammatory disease. Treatment with antibiotic Bethanechol improves symptoms in association with a decrease in the abnormal calcification and enhancement.[4]
Prolyl Endopeptidase Inhibitor 1 (Boc-Pro-prolinal) is a potent prolyl endopeptidase (PEP; PE) inhibitor, with a Ki value of 15 nM. Prolyl Endopeptidase Inhibitor 1 has anti-amnesic effect[1].
M1145, a chimeric peptide, is a selective galanin receptor type 2 (GAL2) agonist, with a Ki of 6.55 nM. M1145 shows more than 90-fold higher affinity for GAL2 over GAL1 (Ki=587 nM) and a 76-fold higher affinity over GalR3 (Ki=497 nM). M1145 has an additive effect on the signal transduction of galanin[1].
GSK189254A (GSK189254) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.
Budipine is an antiparkinsonian agent.
Isonaringin shows anti-Alzheimer’s activity by inhibiting AChE[1].
Rosiridin, which is isolated from Rhodiola rosea L., inhibits MAO A and MAO B with potential beneficial effect in depression and senile dementia. Rosiridin shows an inhibition of 83.8% against MAO B at 10 μM (pIC50=5.38)[1].
SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC50 of 97 nM.
2-Methylthioadenosine diphosphate trisodium is a potent purinergic P2Y receptors agonist, with EC50s of 19, 6.2, and 5 nM for human P2Y13, mouse P2Y13 and human P2Y12, respectively. 2-Methylthioadenosine diphosphate trisodium has pEC50s of 8.29 and 5.75 for human P2Y1 and rat P2Y6, respectively. 2-Methylthioadenosine diphosphate trisodium induces platelet aggregation and shape change, and inhibits cyclic AMP accumulation in platelets exposed to prostaglandin E1[1][2][3].
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect[1][2].