BRL-52656 is a blood-brain barrier (BBB)-penetrable KOR receptor agonist that exhibits a biphasic effect. At low doses, BRL-52656 decreases blood pressure, whereas high doses have the opposite effect in spontaneously hypertensive rats. Additionally, BRL-52656 induces water diuresis by inhibiting the secretion of vasopressin (AVP).

CJ-17493 is a neurokinin-1 (NK1) receptor antagonist, with a Ki of 0.2 nM. CJ-17493 shows moderate affinity for the verapamil-binding site of L-type Ca2+ channels (IC50 = 164 nM) and site 2 of sodium channels (IC50 = 48 nM). CJ-17493 can be used for the study of neurological diseases.

DL-017 is a Quinazoline derivative. DL-017 shows inhibitory constants of approximately 0.90 nM for α1-adrenergic receptors and 404 nM for Na+ channels. DL-017 exerts antihypertensive effect.

BMS-210285 is a highly selective agonist for the β3 receptor. BMS-210285 can be studied for obesity and type 2 diabetes research.

CB2R ligand-1 (Compound L14) is a selective Cannabinoid type 2 receptor (CB2R) ligand with a with Ki of 0.16  nM for CB2R over CB1R. CB2R ligand-1 as be used as a tracer for positron emission tomography (PET) imaging of neurodegenerative diseases, inflammation and cancer.

UVI3502 is a cannabinoid receptor 1 (CB1) antagonist with an IC50 value of 4641 nM for CB1 and approximately 16200 nM for CB2. UVI3502 blocks Gi/o protein coupling induced by the agonist CP55,940. UVI3502 is promising for research of endocannabinoid system-related diseases in the central nervous system (such as cognitive impairment and neurodegenerative diseases).

ST171 is a bitopic 5-HT1AR agonist with an Ki of 0.41  nM. ST171 selectively activates Gi/o signaling pathway and inhibits 5-HT1AR-mediated cAMP accumulation without Gs activation and marginal β-arrestin recruitment. T171 reduces hypersensitivity in chronic neuropathic and inflammatory pain mice model. ST171 can be used for pain research.

IP-66 is a potent postsynaptic alpha-receptor antagonist. IP-66 can be used for the research of cardiovascular disease, such as hypertension.

5-HT2AR ligand 1 (Compound 2 cis) is a 5-HT2AR ligand with nanomolar affinity for 5-HT2AR (Ki: 32 nM). 5-HT2AR ligand 1 is capable of inducing β-arrestin 2 recruitment. 5-HT2AR ligand 1 can be used in the research of neurological diseases.

β-Blocker B-24/76 is a beta adrenoceptor blocker. β-Blocker B-24/76 exhibits beta 1-adrenoceptor blocking and beta 2-adrenoceptor stimulating properties. β-Blocker B-24/76 can suppress the increased ornithine decarboxylase activity in hypertrophied hearts. β-Blocker B-24/76 can be used for the research of cardiovascular disease.

Dopamine D3 receptor ligand-6 (Compound 196476) is a selective dopamine D3 receptor (D3) antagonist. Dopamine D3 receptor ligand-6 is promising for research of substance use disorders (such as opioid and psychostimulant addiction).

L-759656 is a selective cannabinoid CB2 receptor agonist, with the Ki of 11.8 nM for the human CB2 receptor. L-759656 potently inhibits Forskolin-stimulated cyclic AMP production in Chinese Hamster Ovary (CHO) cells, with an EC50 of 3.1 nM. L-759656 can be used for the study of immune-related diseases and inflammatory diseases.

(±)-WB 4101 is a highly selective α1-adrenergic receptor antagonist. (±)-WB 4101 blocks norepinephrine-induced vascular smooth muscle contraction to exert antihypertensive and benign prostatic hyperplasia (BPH)-relieving effects. (±)-WB 4101 is promising for research of hypertension and BPH.

F-14258 is a 5-HT1B/1D receptor agonist. F-14258 can achieve receptor specific analgesia through local administration. F-14258 can be used for research on ear pain.

TGF-8027 is a selective 5-HT2A agonist that can cross the blood-brain barrier. TGF-8027 exhibits EC50s of 3.3 nM, 160 nM and 7600 nM against 5-HT2A, 5-HT2C and 5-HT2B and exhibits EC50s against mouse 5-HT2A and mouse 5-HT2C of 14 and 210 nM. TGF-8027 can induce a head-shaking response in mice. TGF-8027 can be used to study diseases that target the 5-HT2A receptor (such as depression).

Y-36912 is an orally active, highly selective and affinity 5-HT4 receptor agonist (Ki = 1.5 nM). Y-36912 can accelerate gastric emptying and increase bowel frequency and stool weight. Y-36912 can be used for research on gastrointestinal conditions.

BRL 35135 is a potent and selective β3-adrenergic receptor agonist. BRL 35135 can dose dependently increase energy expenditure, reduce weight, and only reduce fat without reducing muscle protein. BRL 35135 can significantly improve glucose tolerance and insulin sensitivity. BRL 35135 can be used to study metabolic conditions such as obesity and diabetes.

CP-99994 is a Tachykinin neurokinin 1 (NK-1) receptor antagonist with a Ki of 0.25 nM. CP-99994 prevents colorectal sensitization in the context of visceral hypersensitivity. CP-99994 reduces colorectal hypersensitivity induced by acetic acid injections in a model of bladder-colon cross-sensitization. CP-99994 hydrochloride attenuates the neuroglial interactions and MAPK-p38 phosphorylation associated with visceral hypersensitivity.

SB 247083 is a selective, competitive and orally active endothelin-A receptor antagonist with a Ki of 0.41 nM. SB 247083 shows a Ki of 467 nM to endothelin-B receptor. SB 247083 shows a Kb of 3.5 nM for ET-1-induced contraction of rat aorta. SB 247083 can be used for the research of cardiovascular disease.

BU08028 is a dual-functional agonist that targets both the μ-opioid peptide receptor (MOP) and the neuropeptide FQ receptor (NOP). BU08028 activates the inhibitory G protein (Giα), thereby inhibiting the activity of adenylate cyclase (AC), resulting in a decrease in intracellular second messenger cyclic adenosine monophosphate (cAMP) levels, and suppressing the generation and transmission of pain signals. BU08028 can take effect within 30 minutes in mouse models of neuropathic pain and inflammatory pain, and its analgesic effect can last for up to 24 hours. BU08028 has excellent safety, no addiction, respiratory depression, or side effects. BU08028 can be used for pain research.

MW073 is a highly selective and orally active 5-HT2BR antagonist (IC50 =70 nM). MW073 exerts its effects by concentration-dependently inhibiting receptor activity and β-arrestin-1 recruitment. MW073 ameliorates synaptic plasticity and behavioral deficits, including aggression, in Alzheimer’s disease (AD) mouse models. MW073 can be used for Alzheimer’s disease (AD) research[1][2].

Elzasonan (CP-448187) is a 5-hydroxytryptamine1B receptor antagonist. Elzasonan is used in research on depression.

rel-Asenapine (rel-Org 5222) hydrochloride is a relative configuration of Asenapine hydrochloride. Asenapine (Org 5222) hydrochloride, an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine hydrochloride can be used in the research of schizophrenia and bipolar disorder.

Anisodine (Daturamine) is a neuroprotective compound that reduces exacerbated M1, M2, M4, and M5 receptor expression in brain tissues under hypoxia/reoxygenation conditions. Anisodine inhibits calcium ion influx and reactive oxygen species (ROS)levels. Anisodine leads to decreased aspartate levels during hypoxia.

BRL-41992 is a selective α₂B-adrenergic receptor antagonist. BRL-41992 exhibits 94-fold higher selectivity for the α₂B-receptor than for the α₂A-receptor with Kᵢ values in neonatal rat lung tissue (expressing the α₂B-receptor) and in human platelet membranes (expressing the α₂A-receptor) of 1.1 and 103.3 nM. BRL-41992 can be used to verify the functional differences of α₂ receptor subtypes.

PD 128483 is a selective dopamine autoreceptor agonist. PD 128483 can be used for the research of neurological disease.

NBI-75043 is an antagonist of H1 receptor.

1-Naphthyl U-47700 is an α-isomer. 1-Naphthyl U-47700 is a racemic mixtures of the trans-isomers [R,R and S,S]. 1-Naphthyl U-47700 activates MOR in a concentration-dependent manner (EC50 > 23 μM).

L 689660 maleate, a cholinomimetic agent, is a selective M1 and M3 muscarinic receptors agonist. L 689660 maleate is a potent M1 muscarinic receptor full agonist in the rat superior cervical ganglion (pEC50 of 7.3). L 689660 maleate is a potent M3 receptors agonist in the guinea-pig ileum myenteric plexus-longitudinal muscle or in trachea (pEC50 of 7.5 and 7.7, respectively).

CGS 22652 is a potent thromboxane A2 receptor antagonist. CGS 22652 has selective thromboxane A2 synthase inhibitory properties. CGS 22652 can be used in the research of coronary artery thrombosis.