nAChR Modulator

PAM-2 is a potent, orally active, CNS-penetrant selective α7 nAChR positive allosteric modulator (human α7 nAChR EC₅₀: 39 μM, rat α7 nAChR EC₅₀: 12 μM) with anti-nociceptive and anti-inflammatory activity. PAM-2 exhibits selectivity over α9α10 nAChR (IC₅₀ = 174 μM) and Ca_V2.2 channel (IC₅₀ = 89 μM). PAM-2 decreases Streptozotocin (STZ) (HY-13753)- and Oxaliplatin (HY-17371)-inducned nuroparhic pain in mice by α7 nAChR potentiation. PAM-2 can be used for the research of neuropathic pain.

Aniracetam (Ro 13-5057) is an orally active neuroprotective agent, possessing nootropics effects. Aniracetam potentiates the ionotropic quisqualate (iQA) responses in the CA1 region of rat hippocampal slices. Aniracetam also potentiates the excitatory post synaptic potentials (EPSPs) in Schaffer collateral-commissural synapses. Aniracetam can prevents the CO₂-induced impairment of acquisition in hypercapnia model rats. Aniracetam can be used to research cerebral dysfunctional disorders.

Phenylpiracetam (Carphedon) is a positive allosteric modulator of nicotinic acetylcholine receptors (nAChR) with an IC₅₀ of 5.86 μM. Phenylpiracetam is applicable to studies on scopolamine (Scopolamine) (HY-N0296)-induced amnesia, depression and immune stress.

Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a K_i of 37 pM.

N-Biotinyl p-aminophenyl arsenic acid is a bifunctional reagent that can bind to both streptavidin and dithiols. N-Biotinyl p-aminophenyl arsenic acid decreases the Rbungarotoxin-binding sites in reduced Torpedo nicotinic receptors (IC₅₀ is 10-300 nM), and protects the receptor from irreversible alkylation by bromoacetylcholine.

TQS is a α7 nicotinic acetylcholine receptor (nAChR) positive allosteric modulator. TQS can be used for the research of neuroinflammatory pain.

S-(+)-Mecamylamine (hydrochloride) is a neuronal nicotinic receptor modulator with antidepressant activity.

Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2, α2β4, α4β2, α4β4, (α4β2)₂α4 and (α4β2)₂β2 EC₅₀ ranges from 0.1-0.6 μM. Br-PBTC acts from the c-tail of an α subunit.

Spinosyn J is a non-competitive insect nicotinic acetylcholine receptor (nAChR) and γ-aminobutyric acid (GABA) receptor modulator with insecticidal activity. Spinosyn J is promising for research of agricultural pests.

Tebanicline tosylate, an analogue of epibatidine, is a neuronal nicotinic acetylcholine receptor agonist. Tebanicline tosylate exhibits potent antinociceptive effects and has a high affinity for the α4β2 neuronal nicotinic acetylcholine receptor subunit in the central nervous system.

α7 nAChR modulator-3 (Compound 6p) is a α7 nAChR positive allosteric Modulator with a IC₅₀ value of 1.3 μM. α7 nAChR Modulator-3 can be used to inhibit auditory gating defects in a mouse schizophrenic model.

GSK575594A is a modulator of the nicotinic acetylcholine receptor (nAChR) in Ascaris suum. GSK575594A enhances muscle contractions induced by acetylcholine (ACh) by binding to the allosteric binding site between subunits within the transmembrane domain of nAChR. At a concentration of 3 μM, GSK575594A significantly increased the contraction induced by ACh in Ascaris suum (E_max increased from 1.19 g to 1.51 g). GSK575594A may be used in research within the field of antiparasitic studies.

DMAB-anabaseine dihydrochloride is a selective nicotinic α7 receptor partial agonist and an α4β2 nAChR antagonist. DMAB-anabaseine dihydrochloride shows cognition-enhancing effects.

α7 nAChR Modulator-2 (Compound 7b) is a α7 nAChR positive allosteric modulator (PAM) with an EC₅₀ of 2.1 μM. α7 nAChR Modulator-2 can be used for the research of cognitive disorders.