Cebranopadol hemicitrate is an analgesic NOP and opioid receptor agonist with Kis/EC50s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively. Cebranopadol hemicitrate can be used for acute and chronic pain study.

BU72 is a highly potent and long-acting agonist of μ and κ opioid receptors, and also has a partial agonist effect on δ opioid receptors (EC50 values are 0.054, 0.033, and 0.58 nM, respectively). BU72 has a strong and long-lasting analgesic effect, which is mainly mediated by μ opioid receptors. BU72 has a long-lasting activity and can partially reverse the analgesic effect of morphine. BU72 can be used in the study of opioid dependence.

Bromadoline is a utopioid with antinociceptive activity in rodents.

Bromadol is an opioid.

BPRMU191 is a μ-opioid receptor (MOR) modulator that converts small-molecule morphinan antagonists into G protein-biased MOR agonists, thereby inducing MOR-dependent activation and analgesic effects. Co-administration of BPRMU191 with morphinan antagonists provides analgesia while reducing side effects such as gastrointestinal dysfunction, antinociceptive tolerance, and dependency-related adverse effects. BPRMU191, in combination with morphinan antagonists, offers a potential strategy for studying severe pain management and G protein-coupled receptor modulation.

BNTX (7-Benzylidenenaltrexone) maleate is a δ1-opioid receptor antagonist with the Kis of 0.1, 10.8, 13.3, and 58.6 nM for δ1, δ2-, μ-, and κ-opioid receptor, respectively. BNTX maleate shows antinociceptive activity.

Bipiperidinyl 4-ANPP is structurally similar to known opioids.

AZ 12488024 (AZD7268) is a SNC80.

AP-238 is a a new synthetic opioid (NSO), and acts as an agonist for μ-opioid receptor (MOR) with an EC50 of 248 nM. AP-238 exhibits analgesic activity.

Alvimopan metabolite hydrochloride is a peripherally restricted Opioid Receptor antagonist that inhibits the amplitude of electrically evoked contractions and spontaneous mechanical activity in guinea pig ileum.

Allyphenyline oxalate (compound 9) can enhance the analgesic effect of Morphine. The pKi values ​​of Allyphenyline for α2A, α2B and α2C are 7.24, 6.47 and 7.07, respectively.

AH-8533 is a opioid agent.

AH 7959 is an orally active N-substituted cyclohexyl methyl benzamide compound that has analgesic effects, the oral and subcutaneous ED50 of AH 7959 in mice is greater than 1 g/kg.

5′-Guanidinonaltrindole (GNTI) is a selective kappa opioid receptor antagonist.

3-Carboxamidonaltrexone (example 32) is a opioid receptor binding compound with Ki values of 1.9 nM, 110 nM, and 22 nM for μ-opioid receptor, δ-opioid receptor, and K-opioid receptor, respectively.

3,4-Difluoro U-50488 hydrochloride is a utopioid.

3,4-Difluoro propyl U-47700 is a utopioid.

3,4-Difluoro isopropyl U-47700 is a utopioid.

2-Naphthyl U-47700 is a utopioid.

2,4-Difluoro U-48800 hydrochloride is a utopioid.

(S)-MCOPPB is the S-form of MCOPPB.

(+)-Norpropoxyphene maleate is an opioid metabolite and is a metabolite of Propoxyphene.

(-)-9-Hydroxycorynantheidine (9-O-Desmethyl mitragynine), the 9-demethyl analogue of Mitragynine, is a selective and partial agonist of μ-opioid receptor. (-)-9-Hydroxycorynantheidine inhibits electrically stimulated twitch contraction in guinea-pig ileum.

SR 142948-C3-NHMe is the methylated SR 142948.

SBI-810 hydrochloride is a functionally selected β-arrestin-biased neurotensin receptor 1 (NTSR1) allosteric modulator. SBI-810 hydrochloride modulates NTSR1 G protein signaling in a G protein-specific manner in the presence of the endogenous ligand, neurotensin (NT). SBI-810 hydrochloride fully antagonizes NT-induced activation of Gq, partially antagonizes NT-induced activation of Gi1 and is permissive of NTSR1 activation of GoA and G12.

SBI-810 is a functionally selected β-arrestin-biased neurotensin receptor 1 (NTSR1) allosteric modulator. SBI-810 modulates NTSR1 G protein signaling in a G protein-specific manner in the presence of the endogenous ligand, neurotensin (NT). SBI-810 fully antagonizes NT-induced activation of Gq, partially antagonizes NT-induced activation of Gi1 and is permissive of NTSR1 activation of GoA and G12.

WIN 62577 is a species-selective tachykinin NK1 receptor antagonist. WIN 62577 is also an allosteric enhancer with micromolar potency at M3 receptors. WIN 62577 exhibits potent antiviral activity against SARS-CoV-2.

Osanetant (SR142801) monohydrochloride is a selective NK3 receptor antagonist. Osanetant monohydrochloride produces anxiolytic- and antidepressant-like effects.

CP 122721 is an orally active NK1 receptor antagonist. CP 122721 attenuates cisplatin-induced vomiting in ferrets (ID50: 0.08 mg/kg). CP 122721 inhibits kainate (KA)-induced seizure activity and CA1 neuronal cell death in rats. CP 122721 is useful in the study of depression, asthma, and irritable bowel syndrome (IBS).

ASN-1377642 is a NK1 receptor antagonist with a Ki value of 251 nM. ASN-1377642 shows antitumor action in breast cancer cells with NK1R-Tr high expression.