Endocrinology/Hormones

(Val3,Pro8)-Oxytocin functions primarily as a Gq-dependent pathway agonist and exhibits secondary activity as a reduced efficacy agonist for β-arrestin

CSD-CH2(1,8)-NH2 is a selective and competitive kappa-opioid receptor (KOR) antagonist with a K i of 6.8 nM.

DALDA TFA is a potent, μ-opioid receptor agonist exhibiting high selectivity and an affinity constant (K i) of 1.69 nM.

AH 8529 is an orally active opioid compound with analgesic properties.

N-Phenethylnoroxymorphone is an opioid compound that can enhance morphine-induced analgesia in rats. It is used in the research of neurological disorders.

KOR agonist 3 (Compound 5) is an agonist of the κ opioid receptor (κOR) with an EC50 of 0.88 nM. It also exhibits some activation of μOR, with an EC50 of 720 nM. However, KOR agonist 3 does not activate δOR at concentrations below 1 μM. Its ability to recruit β-Arrestin-2 is lower than that of U50488.

Pro8-Oxytocin, a modified oxytocin (OXT) ligand, elicits more potent and efficacious responses at primate OXTR and induces stronger behavioral effects compared

Corynantheidine ((-)-Corynantheidine) is a partial agonist of the mu opioid receptor (MOR) and demonstrates MOR-dependent analgesic effects in mice.

AH 7959 is an orally active N-substituted cyclohexylmethylbenzamide compound that exhibits analgesic properties. In mice, the ED50 for oral and subcutaneous administration of AH 7959 exceeds 100 mg/kg.

Dynorphin B (1-9), a neuropeptide and the N-terminal cleavage product of dynorphin B, has its formation inhibited by N-ethylmaleimide (NEM), a non-selective

AP-238 is a novel synthetic opioid (NSO) that acts as an agonist for the μ-opioid receptor (MOR), with an EC50 of 248 nM. Additionally, AP-238 exhibits analgesic properties.

4-Hydroxy-1-(2-phenylethyl)piperidine is a synthetic ligand for muscarinic acetylcholine receptors (mAChR) or non-opioid intracellular sigma-1 receptors (σ1 receptors). It serves as a metabolite of the opioid compounds furanylfentanyl and 4-fluoroisobutyryl fentanyl (FIBF).

β-Endorphin (1-27) (human) is an opioid antagonist that selectively binds to μ-, δ-, and κ-opioid receptors, with dissociation constants (Kis) of 5.31, 6.17,

PF-06655075 (TFA) is the trifluoroacetic acid (TFA) salt of PF-06655075, a novel, non-brain-penetrant oxytocin receptor agonist that exhibits enhanced

(1S,2R)-2-PCCA is a novel and potent small molecule GPR88 receptor agonist with an EC50 value of 3 nM in the non-cellular system and 603 nM in the cellular

Piperidylthiambutene hydrochloride is an opioid compound that exhibits analgesic effects in animal models.

DBPR116 is a prodrug of BPRMU191 that can penetrate the blood-brain barrier. It significantly enhances the delivery efficiency of drugs targeting the central nervous system. When combined with the antagonist Naltrexone, DBPR116 demonstrates superior safety and analgesic effects compared to morphine in various in vivo pharmacological studies, including thermal pain models, cancer pain models, constipation, sedation, psychological dependence, heart rate, and respiratory frequency. As a strategy for peripheral administration, DBPR116 effectively alleviates pain while reducing adverse effects, showing promise as a safer opioid analgesic.

PU-WS13 hydrobromide is a GRP94 inhibitor with anti-inflammatory activity and inhibits the proliferation of M2-like macrophages in mouse TNBC tumors.

R-6890 is an opioid compound with analgesic properties.

AH 8532 is an opioid compound with analgesic effects and is effective in inhibiting the quinone-induced writhing response in mice, with an oral ED50 of 16 mg/kg.