nAChR|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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nAChRs (nicotinic acetylcholine receptors) are neuron receptor proteins that signal for muscular contraction upon a chemical stimulus. They are cholinergic receptors that form ligand-gated ion channels in the plasma membranes of certain neurons and on the presynaptic and postsynaptic sides of theneuromuscular junction. Nicotinic acetylcholine receptors are the best-studied of the ionotropic receptors. Like the other type of acetylcholine receptor-the muscarinic acetylcholine receptor (mAChR)-the nAChR is triggered by the binding of the neurotransmitter acetylcholine (ACh). Just as muscarinic receptors are named such because they are also activated by muscarine, nicotinic receptors can be opened not only by acetylcholine but also by nicotine —hence the name "nicotinic".

Cat. No.	Product Name	CAS No.	Information
H9510	CP-601927	357425-02-6	CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist with Ki values of 1.2 nM and EC50 values of 2.6 μM; CP-601927 shows good brain penetration and antidepressant-like properties.
H9350	Simpinicline	753015-44-0	Simpinicline is a novel small molecule that modulates the activity of the alpha3beta4 and other neuronal nicotinic receptors (NNRs) with Ki value of 17 nM and in human α4β2 and Ki of 34 nM in rat α4B2; The alpha3beta4 NNR is located throughout the gastrointestinal tract and, when modulated, is believed to increase cholinergic tone, which in turn leads to increased motility.
H9349	Ropanicant hydrochloride	2414674-71-6	Ropanicant hydrochloride(SUVN-911) is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity.
H9348	Ropanicant	2414674-70-5	Ropanicant(SUVN-911) is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity.
H8605	PSEM 89S TFA	1336913-03-1	PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively.
H4580	ZSET1446	887603-94-3	A small molecule cognitive enhancer that potentiates acetylcholine-mediated facilitation of inhibitory synaptic transmission in the hippocampal neurons; increases the extracellular ACh in the cortex and hippocampus and enhances nicotine-stimulated ACh release in the hippocampus in normal rats, without affecting nAChRs.
H4579	RO 5126946	1137233-79-4	A novel potent, selective, orally bioavailable and brain-penetran α7nAChR positive allosteric modulator with EC50 of 60 nM; shows excellent selectivity over α4β2nAChR and 5-hydroxytryptamine 3 receptors; enhances α7nAChR synaptic transmission and positively modulates GABAergic responses; improves associative learning in a scopolamine-induced deficit model of fear conditioning in rats, potentiates nicotine's effects on fear memory in vivo.
H4578	RJR-2403 oxalate	220662-95-3	RJR-2403 (Rivanicline, Metanicotine) is a potent, selective neuronal nicotinic ACh (nAChR) agonist with high affinity to rat brain cortex (Ki=26 nM), does not significantly activate muscle type nAChRs or muscarinic receptors; RJR-2403 is comparable to nicotine in activating rat thalamic synaptosomes with EC50 of 732 nM; significantly improves passive avoidance retention after scopolamine-induced amnesia and enhanced both working and reference memory in rats, also demonstrates greatly reduced cardiovascular effects; exerts its antinociceptive effect via nicotinic rather than either opioid or muscarinic mechanisms.
H4577	RJR-2403 hemioxalate		RJR-2403 (Rivanicline, Metanicotine) is a potent, selective neuronal nicotinic ACh (nAChR) agonist with high affinity to rat brain cortex (Ki=26 nM), does not significantly activate muscle type nAChRs or muscarinic receptors; RJR-2403 is comparable to nicotine in activating rat thalamic synaptosomes with EC50 of 732 nM; significantly improves passive avoidance retention after scopolamine-induced amnesia and enhanced both working and reference memory in rats, also demonstrates greatly reduced cardiovascular effects; exerts its antinociceptive effect via nicotinic rather than either opioid or muscarinic mechanisms.
H4576	RJR-2403	15585-43-0	RJR-2403 (Rivanicline, Metanicotine) is a potent, selective neuronal nicotinic ACh (nAChR) agonist with high affinity to rat brain cortex (Ki=26 nM), does not significantly activate muscle type nAChRs or muscarinic receptors; RJR-2403 is comparable to nicotine in activating rat thalamic synaptosomes with EC50 of 732 nM; significantly improves passive avoidance retention after scopolamine-induced amnesia and enhanced both working and reference memory in rats, also demonstrates greatly reduced cardiovascular effects; exerts its antinociceptive effect via nicotinic rather than either opioid or muscarinic mechanisms.

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