heteromeric

NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) that binds with high affinity to heteromeric α3β4 and α4β2 nAChRs, displaying β-subunit preference and no activation at α4-containing receptors. The maximal efficacy of NS3861 depends on the ligand-binding domain, and a serine to threonine substitution in the principal subunit may explain the lack of activation at α4-containing receptors.

E0714 is a blood-brain barrier-permeable, selective Kv7.2 potassium channel activator, with EC50 values of 1.90 μM for the homomeric Kv7.2 channel and 0.021 μM for the heteromeric Kv7.2/7.3 channel. It exhibits anticonvulsant activity and is applicable in epilepsy-related research.

CAY10680 is a dopamine-sparing, benzothiazinone compound that selectively inhibits both MAO-B activity (IC50 = 34.9 nM in human) and adenosine A2A receptors (Ki = 39.5 nM in human). It demonstrates significantly less potent inhibitory values for other adenosine receptor subtypes (Kis > 1 μM) and MAO-A (IC50 ≥ 10 μM). At 1-20 μM, CAY10680 has been shown to abolish cAMP accumulation in CHO cells transfected with adenosine A2A receptors. In the central nervous system adenosine A2A receptor expression is localized to dopamine-innervated areas where heteromeric complexes are formed with dopamine D2 receptors. Because inhibition of adenosine A2A receptors has been shown to enhance D2 receptor function, the blockade of adenosine A2A receptors has emerged as a potential treatment for Parkinson's disease. An additional strategy in the treatment of Parkinson's disease has been to block the activity of monoamine oxidase B (MAO-B), the enzyme involved in dopamine catabolism.

ASIC blocker (IC50 values are 0.44, 2.1 μM and no effect at rat ASIC1a, ASIC3 and ASIC2a, respectively: IC50 value = 0.12 μM at human ASIC1a with no effect at ASIC2a or ASIC3). Inhibition was also observed at heteromeric ASIC channels (IC50 values are 0.79, 0.87 and 4.5 uM at rat ASIC1a+3, ASIC1a+2a and ASIC2a+3; IC5O values are 0.33 and 0.69 uM at human ASIC1a+2a and ASIC1a+3, with no effect at ASIC2a+3). Attenuates pathophysiological nociceptive behaviors in CFA-inflamed and CCI rats.

BTD is a selective transient receptor potential classical 5 (TRPC5) activator, which activates heteromeric channel complexes formed by TRPC5 and its recent relatives TRPC1 or TRPC4, used for studying neurodegenerative diseases.

RO3 is a selective antagonist of homomeric P2X3 and heteromeric P2X2/3 receptor

VUAA1, an insect odorant co-receptor (Orco) agonist, activates heteromeric and homomeric Orco-containing channels and can disrupt the behaviors of nuisance insects, thus serving as a tool for insect olfactory research [1] [2].

NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs), acting as a partial agonist at α3β4 nAChR and binding with high affinity to heteromeric α3β4 nAChR, with binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively[1].