Nicotinic (α7) Receptors

Alpha 7 (α7) is a subunit of the neuronal nicotinic receptor that can combine to form homomeric receptors. The α7 nAChR is prominent in the hippocampus, found on GABAergic interneurons of stratum oriens and stratum radiatum, and on pyramidal neurones.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
4234 4BP-TQS
Allosteric agonist at α7 nAChR
4341 A 582941
Partial agonist at α7 nAChR
4477 A 844606
Selective α7 nAChR partial agonist
3964 AR-R 17779 hydrochloride
α7-selective agonist
3549 3-Bromocytisine
Potent agonist of α4β4, α4β2 and α7 nACh receptors
2241 DMAB-anabaseine dihydrochloride
Partial agonist at α7 nAChR; also α4β2 antagonist
4557 GTS 21 dihydrochloride
Partial agonist at α7 nAChR
3092 PHA 543613 hydrochloride
Potent and selective α7 nAChR agonist
3134 PHA 568487
α7-selective agonist
2303 PNU 282987
Selective α7 nAChR agonist
3518 S 24795
Partial agonist at α7 nAChR
4441 SEN 12333
α7 nAChR agonist; histamine H3 antagonist
5559 SSR 180711 hydrochloride
Partial agonist at α7 nAChR
2518 TC 1698 dihydrochloride
α7-selective agonist

Antagonists

Cat No Product Name / Activity
2133 α-Bungarotoxin
α7 subtype-selective nAChR antagonist
3405 COG 133
ApoE peptide fragment; α7 nAChR antagonist
3119 α-Conotoxin ImI
α7 and α9 selective nAChR antagonist
1029 Methyllycaconitine citrate
α7 neuronal nicotinic receptor antagonist
1356 MG 624
α7 neuronal nicotinic receptor antagonist
2459 Tropisetron hydrochloride
α7 partial agonist; inhibits α3β4 nAChR. Also potent 5-HT3 receptor antagonist

Modulators

Cat No Product Name / Activity
4571 A 867744
Positive allosteric modulator of α7 nAChR
3837 CCMI
Positive allosteric modulator of α7 nAChR
1260 Ivermectin
Allosteric modulator of α7 nicotinic receptors
4141 LY 2087101
Potentiator of α7 nAChRs
2995 NS 1738
Positive allosteric modulator of α7 nAChR; active in vivo
2498 PNU 120596
Positive allosteric modulator of α7 nAChR; active in vivo
4233 TQS
Positive allosteric modulator of α7 nAChRs

Other

Cat No Product Name / Activity
3091 FR 236924
Enhances α7 nAChR activity; PKCε activator
5156 Ivermectin B1a-d2
Deuterated ivermectin B1a (Cat. No. 1260)

α7 is a subunit of the neuronal nicotinic receptor that can combine to form homomeric receptors. In avian tissue α7α8 heteromers also occur and an association between α7 and β2 subunits has been suggested in the mammalian brain. The α7 nAChR is particularly prominent in the hippocampus, where it is found on GABAergic interneurons of stratum oriens and stratum radiatum, and on pyramidal neurones.

Presynaptic α7 nAChRs are present on glutamate terminals and facilitate transmitter release in various brain regions, including the hippocampus, cortex and ventral tegmental area. Nicotine acting at α7 nAChRs can enhance hippocampal LTP, and α7 nAChRs are associated with attentional processes and working memory. As a consequence, α7 nAChRs are a therapeutic target for treating cognitive impairment, notably in Alzheimer's disease and schizophrenia, and this has prompted the generation of α7 nAChR-selective ligands. The human gene encoding the nicotinic α7 receptor subunit has been localized to chromosome 15 (15q13.3).

External sources of pharmacological information for Nicotinic (α7) Receptors :

    Literature for Nicotinic (α7) Receptors

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    Nicotinic ACh Receptors Scientific Review

    Updated in 2014, this review by Sue Wonnacott summarizes the diverse structure and function of nicotinic acetylcholine receptors and gives an in-depth review of the ligands available for nAChR research. Compounds available from Tocris are listed.

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    Nicotinic (α7) Receptor Gene Data

    Species Gene Symbol Gene Accession No. Protein Accession No.
    Human CHRNA7 NM_000746 P36544
    Mouse Chrna7 NM_007390 P49582
    Rat Chrna7 NM_012832 Q05941