Nicotinic Receptor (nAChRs) Pharmacological Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
α1 (muscle) Human CHRNA1 NM_000079 P02708
Mouse Chrna1 NM_007389 P04756
Rat Chrna1 NM_024485 P25108
α2 (neuronal) Human CHRNA2 NM_000742 Q15822
Mouse Chrna2 NM_144803 Q91X60
Rat Chrna2 NM_133420 P12389
α3 Human CHRNA3 NM_000743 P32297
Mouse Chrna3 NM_145129 Q8R4G9
Rat Chrna3 NM_052805 P04757
α4 Human CHRNA4 NM_000744 P43681
Mouse Chrna4 NM_015730 O70174
Rat Chrna4 NM_024354 P09483
α5 Human CHRNA5 NM_000745 P30532
Mouse Chrna5 NM_176844 Q2MKA5
Rat Chrna5 NM_017078 P20420
α6 Human CHRNA6 NM_004198 Q15825
Mouse Chrna6 NM_021369 Q9R0W9
Rat Chrna6 NM_057184 P43143
α7 Human CHRNA7 NM_000746 P36544
Mouse Chrna7 NM_007390 P49582
Rat Chrna7 NM_012832 Q05941
α9 Human CHRNA9 NM_017581 Q9UGM1
Mouse Chrna9 NM_001081104 NP_001074573
Rat Chrna9 NM_022930 P43144
α10 Human CHRNA10 NM_020402 Q9GZZ6
Mouse Chrna10 NM_001081424 NP_001074893
Rat Chrna10 NM_022639 Q9JLB5
β1 Human CHRNB1 NM_000747 P11230
Mouse Chrnb1 NM_009601 P09690
Rat Chrnb1 NM_012528 P25109
β2 Human CHRNB2 NM_000748 P17787
Mouse Chrnb2 NM_009602 Q9ERK7
Rat Chrnb2 NM_019297 P12390
β3 Human CHRNB3 NM_000749 Q05901
Mouse Chrnb3 NM_173212 Q8BMN3
Rat Chrnb3 NM_133597 P12391
β4 Human CHRNB4 NM_000750 P30926
Mouse Chrnb4 NM_148944 Q8R493
Rat Chrnb4 NM_052806 P12392
δ Human CHRND NM_000751 Q07001
Mouse Chrnd NM_021600 P02716
Rat Chrnd NM_019298 P25110
ε Human CHRNE NM_000080 Q04844
Mouse Chrne NM_009603 P20782
Rat Chrne NM_017194 P09660
γ Human CHRNG NM_005199 P07510
Mouse Chrng NM_009604 P04760
Rat Chrng NM_019145 P18916

Nicotinic Pharmacological Receptor Data

nACh Receptor Subtype α2β4 α7 α3β4
Localisation CNS - Cortex, thalamus, hippocampus,striatum Autonomic ganglia, hippocampus, limbic system, cortex, chick retina Autonomic ganglia, adrenal gland, hippocampus
Tissue Function Synaptic transmission, anti-nociception, anxiolytic, memory Synaptic transmission, auditory gating, memory Synaptic transmission
Key Compounds Ki (nM)
Agonists (±-)Anatoxin A (0789)
(-)-Cytisine (1390)
(±)-Epibatidine (0684)
(-)-Lobeline (1077)
RJR 2403 (1053)
UB 165 (1348)
1.3-4.2
0.14-2.7
0.01-0.05
4-50
26
0.27-0.44
707-1840
1400-3883
20.6-233
11000-13100
36000
2790
ND
56-195
0.38
480
ND
ND
Antagonists Chlorisinamide (1001)
Dihydro-β-erythroidine (2349)
Methylcaconitine (1029)
TMPH (2438)
686000
370*
3700-6100
1400*
ND
ND
0.69-10.3
1000*
ND
23100*
ND
200*

*IC50 values