E913 is a CCR5 antagonist that competes with the binding of antibodies to CCR5 which recognize the C-terminal half of the second extracellular loop (ECL2B) of CCR5. E913 can specifically block the binding of macrophage inflammatory protein-1alpha (MIP-1alpha) to CCR5 (IC50 = 0.002 μM) and MIP-1alpha-elicited cellular Ca2+ mobilization (IC50 = 0.02 μM). E913 inhibits the replication of laboratory and primary R5 HIV-1 strains as well as various multidrug-resistant monocyte/macrophage tropic (R5) HIV-1 (IC50 = 0.03-0.06 μM). E913 can be used for the research of infection, such as HIV-1 infection.

FE100726 (Compound 39) is a Cholecystokinin 2 (CCK2) receptor agonist. FE100726 has a superior binding capacity on CCK2 receptor. FE100726 can induce gastric acid secretion in anaesthetized rat models. FE100726 can be used for diabetes research.

ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders.

DNK-333 is a potent and balanced dual NK1 and NK2 receptor antagonist with IC50 values of 4.8 nM and 5.5 nM, respectively. DNK-333 blocks the Neurokinin A (NKA)-induced bronchoconstriction in asthma.

TKA-731 is an NK1 receptor antagonist. TKA-731 can reverse mechanical hyperalgesia. TKA-731 can be used for research on neuropathic pain.

PD 172760 is a selective D4 receptor antagonist. PD 172760 along with the action of other neurotransmitter receptors may be important in treating psychosis.

Dacemazine (Ahistan) is a phenothiazine derivative that acts as a histamine H1 receptor antagonist. Dacemazine exhibits local anesthetic activity and can alleviate spasms induced by acetylcholine and histamine.

AM11638 is an endocannabinoid analog targeting cannabinoid receptors (CB1 and CB2 receptors) with analgesic effects. AM11638 is promising for research of neurological diseases and inflammation-related diseases.

Luvesilocin (Example 6) is a tryptamine prodrug. Luvesilocin can convert into an active form, acting as a 5HT2A agonist in vivo upon administration. Luvesilocin can be studied in research for mental diorders.

Dopamine D4 receptor ligand 3 (Compound 16) is a dopamine D4 receptor (D4R) antagonist (pKi: 8.86). Dopamine D4 receptor ligand 3 has pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 sensors in HEK-293T cells, respectively. Dopamine D4 receptor ligand 3 inhibits the viability of three human glioma cell lines, U87 MG, T98G, and U251 MG. Dopamine D4 receptor ligand 3 induces ROS production and mitochondrial dysfunction in glioma cells.

SAR216471 is a P2Y12 receptor antagonist. SAR216471 reversibly blocks the binding of 2MeSADP to P2Y12 receptors in vitro with an IC50 of 17 nM. SAR216471 can result in the inhibition of platelet aggregation. SAR216471 exhibits anti-thrombotic activity in rat model. SAR216471 can be studied in research on thrombosis.

CCI17464 is a selective, orally active EP4 agonist. CCI17464 can be used in a Freund's complete adjuvant (FCA) acute rat inflammatory pain model and shows complete reversal of allergic reactions.

RS 93427-007 is an orally active prostacyclin stable mimetic agent. RS 93427-007 can be used for the research of cardiovascular disease, such as atherosclerosis.

Dimephosphon is an anti-inflammatory agent with antihistamine and antiserotonin activities. Dimephosphon helps maintain the conduction function of the spinal cord and reduces the excitability of spinal motor neurons in the area surrounding the lesion. Dimephosphon directly activates lymphatic vessel movement and improves lymphatic circulation. Dimephosphon can be used for the study of inflammatory edema, acute spinal cord injury and lymphatic circulation disorders.

YM-50001 is a potent and selective dopamine D4 receptor antagonist with a Ki 5.62 nM. YM-50001 can be used for the research of neurological disease .

RS-86 is a potent, central acting, and selective muscarinic acetylcholine receptor agonist. RS-86 exhibits typical cholinergic excitatory effects, such as inducing smooth muscle contraction, ganglion depolarization, central hypothermia, etc. RS-86 can be used for research on Alzheimer's disease.

SR 142948 TFA is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 TFA antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 TFA blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 TFA shows blood-brain permeability and can be used in study of psychiatric disorders.

SB-203186 is a highly selective 5-HT4 receptor antagonist. SB-203186 exhibits a potent competitive antagonistic effect, with its pKB value being 8.3 in the isolated right atrium model of piglets. SB-203186 can dose-dependently shift the 5-HT-induced tachycardia curve to the right, and does not inhibit the maximum response. SB-203186 is an efficient 5-HT₄ antagonist in pig and human atria, but has no significant inhibitory effect in rat atria. SB-203186 can be used for the study of diseases such as arrhythmias and abnormal myocardial contraction.

Imitrodast sodium is an inhibitor of thromboxane synthase. Imitrodast sodium can be used in the research of bronchoconstriction.

L-161638 is a potent, selective and orally active AT2 receptor antagonist. L-161638 can be used for the research of cardiovascular disease, such as hypertension.

MDA-19 N-(5-hydroxyhexyl) is a cannabinoid receptor modulator targeting CB1R/CB2R. MDA-19 N-(5-hydroxyhexyl) is used to study neurological diseases, cancer, and pain regulation.

UCSF34 (Compound 54) is a Haloperidol analogue. UCSF34 binds to the human D2L receptor, with an estimated pKi of 7.49. UCSF34 can be used in the research of schizophrenia.

S-0509 is a selective CCKB/gastrin receptor antagonist. S-0509 has a strong anti-secretion effect. S-0509 helps prevent the occurrence of duodenal ulcers.

Mivazerol is a selective α2-adrenoceptor agonist. Mivazerol has an anti-ischemic activity. Mivazerol decreases the spontaneous release of serotonin (5-HT) and significantly inhibits the immobilization stress-induced enhancement of norepinephrine (NE), dopamine (DA) and dihydroxyphenylacetic acid (DOPAC). Mivazerol can be used for myocardial ischemia research.

LY377604 hydrochloride is a human β3-adrenergic receptor agonist with an EC50 of 2.4 nM and also a β1- and β2-adrenergic receptor antagonist.

LY334370 fumarate is the fumarate of LY334370). LY334370 is a selective 5-HT1F receptor agonist with a Ki of 1.6 nM.

IHCH-7179 is a 5-HT receptor modulator. IHCH-7179 can antagonize 5-HT2A receptor and activate 5-HT1A receptor. IHCH-7179 can be used for the research of neurological disease.

MP1202 is a dual-functional agonist of MOR and KOR with EC50s of 0.32 and 0.13  μM for mMOR-1 and mKOR-1, respectively. MP1202 has functional selectivity with reduction of β-arrestin1/2 recruitment but significant activation of G-protein and Gα-subtype at hMOR and hKOR. MP1202 has potent antinociceptive effects without typical opioid side effects, but it shows conditioned place preference and aversion behaviors in subtype-selective opioid KO mice model, promising for analgesia research.

Y-20811 (sodium) is a selective and orally active thromboxane synthetase inhibitor. Y-20811 (sodium) can irreversibly inhibit thromboxane (TX) A2 synthesis. Y-20811 (sodium) can be used for the research of cardiovascular disease, such as thrombosis.

SLV-317 (free base) is an antagonist of the neurokinin-1 receptor with oral activity. SLV-317 (free base) can effective antagonist of substance P-induced effects.