ADD-17014 is a L-Glu antagonist. ADD-17014 impairs presynaptic excitatory amino acid L-Glu neurotransmission. ADD-17014 is a prodrug of its β-amino alcohol metabolite, and the metabolite acts as a NMDA receptor antagonist by binding to the MK-801 site located inside the NMDA receptor or ion channel. ADD-17014 has an anticonvulsant and anti-ischemic activity. ADD-17014 can be used for neurodegenerative diseases like Parkinson’s disease, Alzheimer’s disease and stroke research.

MK-5596 is an efficient, selective and orally active CB1R (IC50 = 1.0 nM, EC50 = 5.8 nM) inverse agonist. MK-5596 has weak hERG inhibitory activity. MK-5596 has strong weight loss and appetite suppression effects. MK-5596 has a certain inhibitory effect on CYP enzymes (CYP3A4: IC50 = 3.3 μM, CYP2C8: IC50 = 11 μM, CYP2C9: IC50 = 18 μM, CYP2D6: IC50 = 6 μM). MK-5596 can be used for research on conditions such as obesity.

GR 175737 is a partial histamine H3 receptor agonist, with an EC50 of 7.8 nM. GR 175737 can be used in the research of inflammatory diseases.

SDZ 208-912 is a dual-action 5-HT1A/2 receptor agonist and dopamine D1 receptor antagonist. SDZ 208-912 exhibits partial dopamine agonism and atypical neurosedative effects in rodent models. SDZ 208-912 can be used in research on neurological disorders such as schizophrenia.

Lergotrile is a potent and orally active dopamine agonist and a prolactin secretion inhibitor. Lergotrile inhibits prolactin release from pituitaries by activating an adenohypophyseal dopamine receptor. Lergotrile has the potential for the research of Parkinson's disease.

Raxlaprazine etomoxil is a small molecule compound with dopamine D2 and D3 receptor modulating activity, which has potential application value in research related to mental illnesses. Raxlaprazine etomoxil exhibits high affinity for human recombinant D2L receptors, with an inhibition constant (Ki) of 1.95 nM. Raxlaprazine etomoxil effectively inhibits forskolin-stimulated cAMP accumulation, with an half maximal effective concentration (EC50) of 3.72 nM in functional activity experiments.

RWJ-68022 (Example 9) is a cyclopentene derivative and a motilin receptor antagonist. RWJ-68022 can compete with motilin and erythromycin for the motilin receptor site. RWJ-68022 can be used in the research of gastrointestinal-related diseases.

SRI-22136 is a Delta Opioid Receptor (DOR) antagonist that can cross blood-brain barrier with a IC50 of 0.42 nM. SRI-22136 does not have agonistic activity but antagonistic activity against DOR, MOR (IC50 = 370 nM), KOR (IC50 = 54 nM) and can avoid addiction/aversion effects. SRI-22136 can effectively inhibit the BACE1 activity induced by DADLE (a DOR agonist)) (IC50 = 120 nM). SRI-22136 prevents completely Alzheimer’s-like pathology in mouse model. SRI-22136 can used for the study of Alzheimer’s disease.

SC-42867 is a PGE2 antagonist. SC-42867 can be metabolized in the liver through oxidative N-dealkylation, aromatic hydroxylation, and binding reactions. SC-42867 can be used for research on metabolic conditions.

RS-79948-197 hemihydrate is a non-imidazoline α2-adrenoceptor antagonist. RS-79948-197 hemihydrate shows Kd values of 0.42 nM, 0.18 nM, 0.19 nM, 0.60 nM, 0.46 nM, and 0.77 nM for rat α2A, rat α2B, rat α2C, human α2A, human α2B, and human α2C, respectively.

NZ-107 is an orally active leukotriene receptor antagonist. NZ-107 can inhibit anaphylaxis reaction. NZ-107 can be used for the researches of inflammation and immunology.

NSC 303861 is an L-glutamine antagonist. NSC 303861 selectively inhibits glutamine dependent enzymes in purine nucleotide synthesis without affecting pyrimidine synthase. NSC 303861 has significant cytotoxicity against liver cancer 3924A cells (LC50 = 6 µM). NSC 303861 can be used for cancer research.

SEP-4199 is a nonracemic 85:15 ratio of Aramisulpride and Esamisulpride. SEP-4199 exhibits significant differences in relative potency at two different receptors (5-HT7R and D2R) compared to the racemate. SEP-4199 exhibits antidepressant effects.

Aramisulpride (hydrochloride) is a 5-HT7 receptor antagonist with a Ki value of 22 nM. Aramisulpride (hydrochloride) is a D2/D3 receptor antagonist with a Ki value of 140 nM for D2R and a Ki value of 13.9 nM for D3R. Aramisulpride (hydrochloride) can be used in psychiatric research.

AD109 is a combination of the selective norepinephrine reuptake inhibitor atomoxetine and the antimuscarinic agent aroxybutynin. AD109 shows orally active significantly and reduce the apnea–hypopnea index.

AZD-2327 is a potent and selective δ-opioid receptor agonist. AZD-2327 binds to the human opioid receptor (Ki = 0.49 and 0.75 nM and EC50 = 24 and 9.2 nM at the C27 and F27 isoforms, respectively). AZD-2327 shows selectivity of >1000-fold over the human μ- and κ-opioid receptor subtypes as well as >130 other receptors and channels. AZD-2327 exhibits antidepressant and anxiolytic activities and can be used for the research of neurological disease.

CGS 15873A is an orally active benzopyranopyridine derivative. CGS 15873A has selective dopamine receptor activation activity. CGS 15873A can be used for research on schizophrenia or Parkinson's disease.

CQP-201403 is a dopamine receptor agonist. CQP-201403 can be used for the research of neurological disease.

ORG 31433 is an orally active peptide related to the ACTH-(4-9) analog ORG 2766. ORG 31433 shows neuroprotective effect.

1-Hexadecyl lysophosphatidic acid (1-Hexadecyl LPA) sodium, an ether analog of lysophosphatidic acid (LPA), is a LPA receptor activator.

(Z)-Flupenthixol decanoate is the cis form of Flupenthixol decanoate. (Z)-Flupenthixol decanoate is a potent dopamine D1/D2 receptor antagonist. (Z)-Flupenthixol decanoate shows antipsychotic effect.

BBL454 (Compound 43) is a Cholecystokinin 2B (CCK2B) receptor agonist. BBL454 induces hyperactivity and improves memory in rat models while it has weak activity on the peripheral CCK2 receptor and no anxiogenic activity. BBL454 increases gastric acid output in anesthetised rat models. BBL454 can be used for diabetes research.

U-46619 Glycine methyl ester has a modification at the C-1 position of U-46619, which uniquely alter its binding properties to the TP receptor or any of the PGH2-metabolizing enzymes. U-46619 is a stable analog of the endoperoxide PGH2. U-46619 is also an agonist of TP receptor. U-46619 can change the shape of platelet, aggregation and contraction of vascular smooth muscle. U-46619 Glycine methyl ester can be studied in research to explore the inhibition of various enzymes in the arachidonic acid metabolic pathway. U-46619 Glycine methyl ester can also act as a lipophilic prodrug form of U-46619 that alters its distribution and pharmacokinetic properties.

EXP-7711 is a non peptide angiotensin II (Ang II) AT1 receptor antagonist. EXP-7711’s affinity for wild-type AT1 receptor (Ki =180 nM) is lower than peptide antagonists, but higher than losartan (Ki = 12 nM). EXP-7711 can be used for research on cardiovascular conditions.

CR 3834 is a angiotensin-AT1 antagonist. CR 3834 can be used for the research of cardiovascular disease.

Carbaprostacyclin-biotin (cPGI-biotin; Carbacyclin-biotin) is a biotin-bound Carbacyclin (Carbaprostacyclin)). Carbacyclin is a PGI2 analogue, acts as a prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation.

(±)5(6)-EET Ethanolamide is a metabolite of Anandamide generated via oxidation by cytochrome P450 enzymes. (±)5(6)-EET Ethanolamide is also a selective cannabinoid receptor 2 (CB2) agonist. (±)5(6)-EET Ethanolamide has Ki values of 11.4 μM and 8.9 nM for human CB1 and CB2, respectively . (±)5(6)-EET Ethanolamide can be used in research on immunomodulation and neuroinflammation.

P2Y12R ligand-1 (Compound 41) is a high-affinity P2Y12R ligand with a Ki value of 17.1 nM. P2Y12R ligand-1 labeled with [18F] can be used in studies of brain PET imaging.

MRS8454 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR). MRS8454 can significantly enhance the maximum effect of the standard agonist Cl-IB-MECA by approximately 286%-300%, and significantly reduce its EC50 value. MRS8454 effectively enhances the ability of A3AR agonists to inhibit the cAMP accumulation induced by Forskolin. MRS8454 can be used for the development of molecular probes.

YM-358 hydrate (potassium) is an orally active angiotensin II type 1 (AT1)-receptor antagonist. YM-358 hydrate (potassium) can decrease cardiac volume overload. YM-358 hydrate (potassium) can be used for the research of cardiovascular disease, such as hypertension.