subtypes

(R)-Terazosin is an active R-enantiomer of Terazosin and a potent antagonist of α1-adrenoceptor [(α1a, α1b, and α1d-adrenoceptor] with Ki values of 6.51 nM, 1.01 nM, and 1.97 nM, respectively).

Ozanimod (RPC-1063) (RPC1063) is a specific oral S1P Receptor 1 modulator. Ozanimod has been used in trials studying the treatment of Crohn's Disease, Ulcerative Colitis, Multiple Sclerosis, and Relapsing Multiple Sclerosis.

PP7 is a potent inhibitor of PB1-PB2 interaction(IC50 of 8.6 μM).

Kainic acid is an excitatory amino acid receptor agonist (EC50=16.2 μM). Kainic acid is an effective excitatory toxic agent. Kainic acid induces epileptic seizures.

MY-1B is a covalent inhibitor and an inhibitor of RNA methyltransferase NSUN2 (IC50 = 1.3 μM), featuring stereoselectivity, covalent binding to C271 of NSUN2, and the ability to target PSME1, disrupt proteasome regulatory complexes, and downregulate presentation of specific MHC-I subtypes.

(±)-Tazifylline is a selective and long-acting antagonist of histamine H1 receptor. Tazifylline shows much lower affinity for H2 receptors, α- and β-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes.

Deramciclane has high affinity for 5-HT2A and 5-HT2C receptors. It acts as an antagonist in both receptor subtypes and has inverse agonist properties for 5-HT2C receptors, but no direct stimulant agonists.

DFP00173 is a potent and selective aquaporin 3 (AQP3) inhibitor, with an IC50 of approximately 0.1-0.4 μM for both mouse and human AQP3. It demonstrates selectivity for AQP3 compared to homologous AQP subtypes AQP7 and AQP9.

DMCM hydrochloride is a non-selective fully inverse agonist of benzodiazepine. DMCM showed significant differences in human recombinant GABAA αxβ3γ2 receptor subtypes. For α1, α2, α3, and α5 receptors, their Kis were 10 nM, 13 nM, 7.5 nM, 2.2 nM, respectively.

L162389 is an orally active and potent angiotensin II receptor antagonist with a balanced affinity for AT1 and AT2 receptor subtypes that stimulates the conversion of phosphatidylinositol.

SS-208 is a selective inhibitor of HDAC6 (IC50 = 12 nM) with anti-tumor activity. SS-208 shows selectivity over other HDAC subtypes.

BMY-27709 is an influenza virus growth inhibitor with an IC50 value of 3-8 μM against A/WSN/33 virus growth and demonstrates inhibitory activity against certain subtypes of influenza viruses. BMY-27709 acts early in H1 and H2 virus infections by inhibiting hemagglutinin proteins but has no effect on H3 subtype viruses and influenza B/Lee/40 viruses.

MPT0G211 is a highly selective and orally active HDAC6 inhibitor (IC50=0.291 nM) that has neuroprotective effects and has shown anti-metastatic activity in human breast cancer cells. MPT0G211 has 1,000 times more affinity for HDAC6 than other HDAC subtypes. MPT0G211 can cross the blood-brain barrier and could be used to improve tau phosphorylation and cognitive deficits in Alzheimer's disease models.

FiVe1 is a vimentin binding small molecule that promotes the disintegration and phosphorylation of vimentin in the metaphase, leading to mitotic disasters, polynuclearization, and loss of cancer cell dryness. FiVe1 selectively and irreversibly inhibit the growth of mesenchymal transformed breast cancer cells (FOXC2-HMLER cell, IC50=234nM) and soft tissue sarcomas of different histological subtypes.

Oxybutynin chloride (Oxybutynin HCl) is an anticholinergic medication used to relieve urinary and bladder difficulties. It competitively antagonizes the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor.

Proglumide (Binoside) is a cholecystokinin antagonist, which blocks both the CCKA and CCKB subtypes. Proglumide is a drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.

Dacomitinib hydrate (PF 299804) is a highly selective and second-generation small-molecule inhibitor of the pan-epidermal growth factor receptor family of tyrosine kinases. Dacomitinib specifically and irreversibly binds to and inhibits human EGFR subtypes, resulting in inhibition of proliferation and induction of apoptosis in EGFR-expressing tumor cells.

VU0364770 (VU 0364770)(EC50=1.1 μM), a positive allosteric modulator(PAM) of mGlu4, shows insignificant activity at 68 other receptors, including other mGlu subtypes.

BMS-986169 is a high-affinity and selective negative allosteric modulator of the NMDA receptor GluN2B subunit, with an IC50 of 24 nM in oocytes, and exhibits antidepressant-like activity in mice, making it a potential treatment for treatment-resistant depression.

GABAA receptor agent 5 demonstrates antagonist activity across multiple GABAA receptor subtypes, and GABAA receptor agent 5 exhibits IC50 values of 0.24, 0.088, 0.068, 0.33, 0.79, 0.32, 0.079, and 0.051 μM for α1β2δ, α4β1δ, α4β2δ, α6β2δ, α1β2γ2, α2β2γ2, α3β2γ2, and α5β2γ2 receptor configurations, respectively. GABAA receptor agent 5 (compound 018) thereby provides a precise pharmacological tool for characterizing subtype-selective GABAA receptor inhibition and supports mechanistic neuropharmacology studies focused on inhibitory synaptic signaling and therapeutic antagonist development.

B-TPMF is a highly efficient and selective KCa2.1 channel inhibitor with an IC50 of 31 nM, interacting with the serine residue at position 293 to inhibit KCa2.1.

L-838417-D9 is a novel deuterated subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].

BMS641 (BMS-209641) is a selective and potent RARβ agonist with high affinity for RARβ, which synergistically activates RARβ and RARgamma to induce cellular maturation into specialized neuronal subtypes.

Quetiapine (ICI204636) is used for the therapy of schizophrenia, and for the treatment of acute manic episodes associated with bipolar I disorder. The mechanism of quetiapine' action is thought by mediated through antagonist activity at serotonin and dopamine receptors. Specifically, the D1 and D2 dopamine, the α1 adrenoreceptor and α2 adrenoreceptor, and 5-HT1A and 5-HT2 serotonin receptor subtypes are antagonized. Quetiapine also can inhibit the histamine H1 receptor.