TABLE 2.
nAChR Current Types | Putative Subunits Involved | Neuron Types Expressing nAChRs | Choline as Agonist | Cytisine as Agonist | Choline as Antagonist | MLA Inhibition at 10 nM | DHβE Block at 10 µM | MEC Block at 1 µM | Bupropion Block at 1 µM | Nicotine Inhibition | Reference Nos. |
---|---|---|---|---|---|---|---|---|---|---|---|
Type IA | α7 | Hippocampal interneurons; midbrain dopamine neurons; neurons from olfactory bulb and cortex | Full agonist | Yes, IC50 = 37 µM | Full agonist | >95% | 40% | <10% | 0% | IC50 = 100–1,500 nM | 16, 18, 25, 27, 145, 154, 316, 504 |
Type II | α4β2 | Hippocampal SLM interneurons; midbrain dopamine neurons; neurons from thalamus, IPn, and catecholaminergic nucleus | Not an agonist Agonist | Yes, IC50 = 370 µM | Partial agonist | 0% | >95% | ND | 14% | IC50 = 20–125 nM | 16, 18, 504 |
Type III | α3β4β2 | Glutamate axons to hippocampal interneurons; neurons from MHb, IPn, and dorsal medulla | Partial agonist | Yes, IC50 = 15 µM | Full agonist | 0% | 33% | 80% | 54% | IC50 = 13 nM | 16, 18, 527 |
Type IV | α2β4/α4β4 | Neurons from MHb and IPn | ND | ND | Full gonist | 0% | 0% in MHb; 36% at 1 µM | ND | ND | ND | 527 |
Pharmacological classification of nAChRs in the rodent brain slices is based on patch-clamp analysis. ND, not determined; MHb, medial habenula; IPn, interpeduncular nucleus.