M4 mAChR agonist-1 (compound 10a) is a potent M4 mAChR agonist with an EC50 >10 μM for human M4[1].
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].
F13714 fumarate, a selective 5-HT1A receptor biased agonist, shows antidepressant-like properties after a single administration in the mouse model of chronic mild stress[1].
Cytisine is an alkaloid that occurs naturally in several plant genera, such as Laburnum and Cytisus. Cytisine is a partial agonist of α4β2 nAChRs[1], and partial to full agonist at β4 containing receptors and α7 receptors[2]. has been used medically to help with smoking cessation[3].
SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model[1].
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].
A68930, as a dopamine D1 receptor agonist, can be used for the research of bronchiectasis[1].
Iproniazid is a non-selective, irreversible monoamine oxidase inhibitor (MAOI) of the hydrazine class.
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].
DL-Borneol is a racemic mixture of D-Borneol and L-Borneol. DL-Borneol is widely used for the treatment of cardiovascular and cerebrovascular diseases in China.
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].
Duloxetine D3 hydrochloride ((S)-Duloxetine D3 hydrochloride) is a deuterium labeled Duloxetine hydrochloride. Duloxetine hydrochloride is a serotonin-norepinephrine reuptake inhibitor (SNRI) with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD)[1][2].
SB-200646 is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646 is orally active and has electrophysiological and anxiolytic properties in vivo[1][2].
TAT-GluA2 3Y is an inhibitor of AMPA receptor endocytosis. TAT-GluA2 3Y induces increased hind paw withdrawal latencies following thermal and mechanical stimuli in rats. TAT-GluA2 3Y also exhibits antinociceptive effects in a rat model of neuropathic pain. TAT-GluA2 3Y rescues pentobarbital-induced memory retrieval deficits in a rat model of learning and memory.
Ifenprodil tartrate is a novel N-methyl-D-aspartate (NMDA) receptor antagonist that selectively inhibits receptors containing the NR2B subunit.
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
Perzinfotel (EAA-090) is a potent, selective, and competitive NMDA receptor antagonist with neuroprotective effects. Perzinfotel (EAA-090) shows high affinity (IC50=30 nM) for the glutamate site[1][2].
Oxitropium bromide is an mAChR antagonist used as an anticholinergic bronchodilator drug for the treatment of asthma and chronic obstructive pulmonary disease.
Choline-13C2 (chloride) is the 13C labeled Choline chloride[1]. Choline chloride 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[2][3].