Piperilate (Pipethanate) is one of the mixtures of hetrazepine derivative PAF antagonists with anticholinergics, can be used for bronchial asthma research. Piperilate also causes hypotension and rescues mice poisoned by the organophosphates[1][2][3].
L-DOPA (Levodopa) sodium is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA sodium can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA sodium has anti-allodynic effects, and can be used for Parkinson's disease research[1][2][3].
Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities.
Arecaidine hydrochloride, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrochloride is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake[1][2].
Naltrindole hydrochloride is a highly potent and selective non-peptide δ opioid receptor antagonist with a Ki of 0.02 nM.
Fmoc-L-Val-OH-13C5,15N is a 15N-labeled and 13C-labled Pirimicarb. Pirimicarb is a fast-acting selective carbamate insecticide on a wide range of crops including cereals, sugar beet, potatoes, fruits and vegetables. Pirimicarb is an AChE inhibitor and an
CP-135807 is an orally active and selective 5-HT1D agonist (IC50=3.1 nM), bovine). CP-135807 mediates central psychoactivity and can be used in antidepressant research[1][2].
Tau-aggregation-IN-1 (Compound D-519) is a tau441 protein aggregation inhibitor with an IC50 of 21 µM. Tau-aggregation-IN-1 is also a dopamine D2 and D3 receptor agonist[1].
Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent[1].
mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM[1].
Pramipexole (N-Propyl-3,3,3-d3) dihydrochloride is the deuterium labeled Pramipexole. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].
Hemicholinium 3 is a competitive inhibitor of the high affinity choline transporter (HACU) with a Ki value of 25 nM. Hemicholinium 3, a neuromuscular blocking agent which inhibits the synthesis and the release of acetylcholine (ACh)[1]. Hemicholinium 3 inhibits the Epibatidine-evoked contraction and [3H]acetylcholine release with IC50s of 897 nM and 693 nM, respectively[2].
Apomorphine is an orally active agonist of Dopamine receptor. Apomorphine can be used in study Parkinson, biphasic dyskinesias, urinary dysfunction,,dystonia, dyspnoea, anismus and belching[1].
sEH inhibitor-5 (compound D016) is a potent sEH (soluble epoxide hydrolase) inhibitor with an IC50 value of 0.1 nM[1].
Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects[1].
Camylofin is an antimuscarinic, is a smooth muscle relaxant
Lurasidone-d8 is deuterium labeled Lurasidone. Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile[1].
Desoxypeganine (Deoxypeganine), an alkaloid, is a potent and orally active cholinesterase (BChE and AChE) and selective MAO-A inhibitor, with IC50 values of 2, 17, and 2 μM, respectively. Desoxypeganine can be used for alcohol abuse research[1].
Epiboxidine hydrochloride is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine hydrochloride is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418[1].
SPD-473 citrate is a serotonin/dopamine/norepinephrine reuptake inhibitior.
Ziprasidone (CP-88059) mesylate trihydrate is an orally active combined 5-HT and dopamine receptor antagonist[1]. Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM)[1].
Talnetant Hcl(SB 223412 Hcl) is a potent and selective NK3 receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM.IC50 Value: 1.4 nM (hNK-3-CHO binding Ki) [1]Target: NK3 receptorin vitro: In vitro studies demonstrated that 53 is a potent functional antagonist of the hNK-3 receptor (reversal of senktide-induced contractions in rabbit isolated iris sphincter muscles and reversal of NKB-induced Ca2+ mobilization in CHO cells stably expressing the hNK-3 receptor), while in vivo this compound showed oral and intravenous activity in NK-3 receptor-driven models (senktide-induced behavioral responses in mice and senktide-induced miosis in rabbits) [1]. Talnetant has high affinity for recombinant human NK3 receptors (pKi 8.7) and demonstrates selectivity over other neurokinin receptors (pKi NK2 = 6.6 and NK1<4). In native tissue-binding studies, talnetant displayed high affinity for the guinea pig NK3 receptor (pKi 8.5) [3].in vivo: Rectal barostat tests were performed on 102 healthy volunteers, randomized to receive either oral talnetant 25 or 100 mg or placebo over 14-17 days [2]. Talnetant (3-30 mg/kg i.p.) significantly attenuated senktide-induced 'wet dog shake' behaviors in the guinea pig in a dose-dependent manner. Microdialysis studies demonstrated that acute administration of talnetant (30 mg/kg i.p.) produced significant increases in extracellular dopamine and norepinephrine in the medial prefrontal cortex and attenuated haloperidol-induced increases in nucleus accumbens dopamine levels in the freely moving guinea pigs [3].Toxicity: Talnetant had no effect on rectal compliance, sensory thresholds or intensity ratings compared with placebo [2].Clinical trial: Study Of Talnetant Versus Placebo And Risperidone In Schizophrenia. Phase 2
Lycoramine, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine is a potent acetylcholinesterase (AChE) inhibitor[1][2].
L-Phenylalanine-3-13C ((S)-2-Amino-3-phenylpropionic acid-3-13C) is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
AM 374 is an fatty acid amide hydrolase (FAAH) inhibitor. AM 374 inhibits amidase activity with an IC50 value of 13 nM. AM 374 can be used for the research of neurological disease[1][2].
Malathion is an organophosphate parasympathomimetic which binds irreversibly to cholinesterase, is an insecticide of relatively low human toxicity.
STO-609 is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively.
RPR104632 is a specific antagonist of NMDA receptor, with potent neuroprotective properties.