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.

Anthrotainin, a tetracyclic compound, is a substance P binding inhibitor with an IC50 of 3 μM.

(1R,2S,3R)-Aprepitant (Compound ent-4) is a competitive human neurokinin-1 (NK-1) receptor antagonist. (1R,2S,3R)-Aprepitant is promising for research of cancers and postoperative nausea and vomiting.

YM-202074 is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models.

VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801, and has anti-tumor activity.

VU6031545 is a potent mGlu 5 negative allosteric modulator with an IC50 of 15 nM. VU6031545 has excellent brain penetrant and oral bioavailability in rats.