MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC50s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC50 > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder.

(Rac)-MK 0686 is the racemate of MK 0686. MK 0686 is a bradykinin B1 receptor antagonist.

LMD-584 is an agonist of CCR8. LMD-584 is also an analog of LMD-009.

1192U90 is an antipsychotic agent, dopamine D2 receptor antagonist as well as serotonin 5-HT1a receptor agonist. 1192U90 reduces the number of spontaneously firing neurons in the limbic dopamine system.

DuP-532 is an angiotensin type 1 receptor antagonist with potential activity in the suppression of hypertension and heart failure. DuP-532 can react with a range of aryl and heteroaryl halides to form perfluoroalkyl(hetero)arenes in moderate to high yields. Computational studies of DuP-532 suggest that coordination of a second phenyl ring ligand may lower the energy barrier for decarboxylation of perfluorocarboxylates, thereby promoting the perfluoroalkylation reaction.

Carpipramine is an antipsychotic agent that belongs to the iminodibenzyl class. Carpipramine is a potent dopamine antagonist which blocks alpha 1- and alpha 2-adrenoceptors. Carpipramine also has antagonist properties with respect to serotonin (5-ΗΤ2) receptors. Carpipramine exhibits antipsychotic and anti-depressant effects. Carpipramine can be used for the research of neurological disease, such as post-traumatic stress disorder (PTSD) and depression.

UTPU (trisodium) (Compound 19) is a selective P2Y6R agonist with an EC50 of 0.4 μM. UTPU (trisodium) can activate the intracellular calcium signaling pathway mediated by P2Y6. UTPU (trisodium) can be used for the research of inflammation.

GYKI 12743 is a vasoselective, postsynaptic α-adrenoceptor blocker. GYKI 12743 inhibits but does not completely eliminate the cutaneous microcirculatory blood flow reduction evoked by electrical stimulation of the peripheral stump of the cut saphenous nerve in rats. GYKI 12743 can be used for the study of neurological diseases.

Tropapride is a dopamine D2 receptor antagonist. Tropapride can be used for the research of neurological disease.

EXP-6803 is a specific nonpeptide angiotensin II receptor antagonist with antihypertensive activity. EXP-6803 inhibits the contractile response to angiotensin II with a pA2 value of 7.20. EXP-6803 effectively blocks responses to angiotensin I and II while not affecting responses to bradykinin or acetylcholine in guinea pig ileum. EXP-6803 can be used for hypertension research.

ISAM-CG557 is a selective CB2R agonist, with a Ki of 54.6 nM. ISAM-CG557 reduces intracellular ROS levels and caspase activity. ISAM-CG557 exhibits significant MAPK bias and moderate G-protein bias, with CB2R EC50s of 0.60 nM (cAMP), 60.9 nM (β-arrestin) and 0.03 nM (MAPK). ISAM-CG557 exerts potent anti-inflammatory effects by reducing pro-inflammatory cytokines and increasing anti-inflammatory cytokines in cells. ISAM-CG557 can be used for the study of neuroinflammatory and neurodegenerative disorders.

MGS0008 is an orally active and brain-penetrant metabotropic glutamate receptor 2/3 (mGlu2/3) agonist. MGS0008 is promising for research of central nervous system disorders, including schizophrenia, anxiety, and neurodegenerative diseases.

Rp-dUTPαS (tetrasodium) is an isomer of the sulfur-containing nucleoride dUTP-α-S and an agonist of the purinergic P2Y2 receptor. Rp-dUTPαS (tetrasodium) selectively induces inositol phosphate accumulation in P2Y2-expressing 1321N1 cells with an EC50 of 12.5 μM.

20:4 Lyso PI is a selective G protein-coupled receptor GPR55 agonist. 20:4 Lyso PI triggers cell rounding in GPR55-expressing HEK293 cells, with an EC50 value of 10 nM. 20:4 Lyso PI promotes RhoA activation and subsequent ROCK-dependent cytoskeletal rearrangement. 20:4 Lyso PI activates the ERK signaling pathway and elevates intracellular free calcium. 20:4 Lyso PI can be used for the study of immune diseases.

Uridine 5'-O-thiodiphosphate (trisodium) (UDP-β-S (trisodium)) is a purinergic P2Y6 receptor agonist. Uridine 5'-O-thiodiphosphate (trisodium) selectively induces accumulation of inositol phosphates in 1321N1 cells expressing P2Y6 receptors (EC50 = 28 nM). Uridine 5'-O-thiodiphosphate (trisodium) induces DNA synthesis in rat aortic smooth muscle cells.

Rp-UTP-α-S (tetrasodium) is a nucleotide agonist of purinergic P2Y2 and P2Y4 receptors. Rp-UTP-α-S (tetrasodium) can induce inositol phosphate accumulation in P2Y2 or P2Y4 expressing 1321N1 cells with EC50 values of 5.4 and 27 μM.

UDP trisodium (Compound 3), a nucleotide, is a P2Y14 receptor agonist with an EC50 of 160  nM for P2Y14 receptor over the P2Y6 receptor. UDP trisodium can be used for pain, diabetes, cystic fibrosis and other pulmonary diseases research.

1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) (1-Arachidonoyl-sn-glycerol 3-phosphate (sodium)) is a phospholipid with arachifonic acid at the sn-1 position. 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) binds to the LPA2/EDG4 receptor (EC50 of 10 nM). 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) can be found in rat brain as 37% of the arachidoinic acid-containing lysophosphatidic acid species. 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) is the precursor to 1-arachidonoyl glycerol. 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) can prevent TNF-α and IL-6 secretion in wild type LPS-stimulated dendritic cells. 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) reduces differentiation of HT-29 colon carcinoma cells into goblet cells when sodium butyrate is present.

Butopamine is the active R/R stereoisomer butapamine of ractopamine hydrochloride. Butopamine exerts its physiological effects by stimulating β1-adrenergic receptor (β1AR) and β2-adrenergic receptor (β2AR) expressed in skeletal muscle and adipose tissue.

MDAN-21 is a bivalent opioid ligand that contains both μ-opioid receptor agonists and δ-opioid receptor antagonists. MDAN-21 has a strong analgesic effect and does not produce tolerance in mouse studies. MDAN-21 can effectively inhibit the withdrawal of morphine dependent monkeys and alleviate abnormal pain in the study of rhesus monkeys. MDAN-21 can be used for the study of allodynia.

R 116712 is a highly selective and affinity 5-HT4 receptor ligand. R 116712 can prepare isotopic markers.

Naxaprostene is a prostacyclin analogue. Naxaprostene was much more selective for IP receptors and tended towards partial agonism. Naxaprostene inhibits ADP-induced platelet aggregation. It has been shown to prevent rabbit carotid artery thrombosis.

AR-102 isopropyl ester is a second-generation prostaglandin FP agonist. AR-102 isopropyl ester can be studied in research for glaucoma and ocular hypertension.

2-(2-Methoxyphenoxy)ethylamine hydrochloride (Compound 2b) is a mixed agonist/antagonist. 2-(2-Methoxyphenoxy)ethylamine hydrochloride is a5-HT1A receptor partial agonist and a α1-adrenergic receptor antagonist. 2-(2-Methoxyphenoxy)ethylamine hydrochloride can be used for neurological diseases research, such as anxiety, depression and psychosis.

SV119 is a selective sigma-2 (σ₂) receptor ligand (Ki ≈ 5-10 nM). SV119 induces apoptosis in various human cancer cell lines by activating caspase-3 and promoting mitochondrial depolarization. SV119 can enhance the effects of chemotherapeutic agents such as Paclitaxel, increasing their cytotoxicity against tumor cells. SV119 significantly inhibits tumor growth in mouse xenograft models, both alone and in combination. SV119 is useful in the research of cancers such as breast, prostate, and pancreatic cancer.

5-Benzyloxytryptamine (5-BT) is a selective partial agonist for 5-hydroxytryptamine 1D/1B (5-HT1D/1B) receptors with an IC50 value of 40 nM for bovine caudate 5-HT1D and reduced affinity for other receptors (5-HT2 IC50>470 nM). 5-Benzyloxytryptamine inhibits adenylate cyclase to decrease neurotransmitter release and downregulate cAMP signaling. 5-Benzyloxytryptamine is promising for research of neurotransmitter imbalance-related disorders like migraine.

L694247 (TFA) is a selective 5-HT1D agonist with pIC50 values of 10.03, 8.64, 6.42, and 5.66 for 5-HT1D, 5-HT1A, 5-HT1C, and 5-HT1E receptors, respectively.

ZH8659 hydrochloride is a trace amine-associated receptor 1 (TAAR1)-Gq agonist. ZH8659 hydrochloride can be used for the research of neurological disorders.

AR-C66096 is a potent and selective antagonist of the Gi-coupled P2Y12 receptor. AR-C66096 suppresses platelet thrombus stability under physiological flow conditions. AR-C66096 inhibits ADP-induced aggregation in whole blood aggregometry. AR-C66096 can be used for antithrombotic research.

LY-228729 is a selective 5-HT1A receptor agonist. LY-228729 can reduce the rearing frequency of rats and decrease their activity in the central area in the open field test. LY-228729 can reduce the immobility time of rats and increase their swimming time in the forced swim test. LY-228729 can be used in the research of neurological diseases.