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The alpha-7 nicotinic receptor (α7)5 is a type of nicotinic acetylcholine receptor, consisting entirely of α7 subunits [1].
It is located in the brain, where activation yields post- and presynaptic excitation[1], mainly by increased Ca2+ permeability.
Contents |
Ligands
Agonists
- (+)-N-(1-azabicyclo[2.2.2]oct-3-yl)benzobfuran- 2-carboxamide: potent and highly subtype-selective[2]
- PHA-709829: potent and subtype-selective; robust in vivo efficacy in a rat auditory sensory gating model[3]
- A-582941: partial agonist; activates ERK1/2 and CREB phosphorylation; enhances cognitive performance[5]
- TC-1698: subtype-selective; neuroprotective effects via activation of the JAK2/PI-3K cascade, neutralized by angiotensin II AT(2) receptor activation[6]
- SSR180711: partial agonist[7]
- tropisetron: subtype-selective partial agonist; 5-HT3 receptor antagonist[8]
Antagonists
- α-conotoxin ArIB[V11L,V16D]: potent and highly subtype-selective; slowly reversible[9]
- quinolizidine (–)-1-epi-207I: α7 subtype preferring blocker[10]
PAMs
At least two types of positive allosteric modulators (PAMs) can be distinguished.[11]
- PNU-120596 [12]
- NS-1738: marginal effects on α7 desensitization kinetics; modestly brain-penetrant[13]
References
- ^ a b Pharmacology, (Rang, Dale, Ritter & Moore, ISBN 0443071454, 5:th ed., Churchill Livingstone 2003) Page 138.
- ^ Mazurov A, Klucik J, Miao L, et al (2005). "2-(Arylmethyl)-3-substituted quinuclidines as selective alpha 7 nicotinic receptor ligands". Bioorg. Med. Chem. Lett. 15 (8): 2073–7. doi:. PMID 15808471.
- ^ Acker BA, Jacobsen EJ, Rogers BN, et al (2008). "Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl] furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity". Bioorg. Med. Chem. Lett. 18 (12): 3611–5. doi:. PMID 18490160.
- ^ Walker DP, Wishka DG, Piotrowski DW, et al (2006). "Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl amides as alpha7 nicotinic acetylcholine receptor agonists". Bioorg. Med. Chem. 14 (24): 8219–48. doi:. PMID 17011782.
- ^ Tietje KR, Anderson DJ, Bitner RS, et al (2008). "Preclinical characterization of A-582941: a novel alpha7 neuronal nicotinic receptor agonist with broad spectrum cognition-enhancing properties". CNS Neurosci Ther 14 (1): 65–82. doi:. PMID 18482100.
- ^ Marrero MB, Papke RL, Bhatti BS, Shaw S, Bencherif M (2004). "The neuroprotective effect of 2-(3-pyridyl)-1-azabicyclo[3.2.2]nonane (TC-1698), a novel alpha7 ligand, is prevented through angiotensin II activation of a tyrosine phosphatase". J. Pharmacol. Exp. Ther. 309 (1): 16–27. doi:. PMID 14722323.
- ^ Biton B, Bergis OE, Galli F, et al (2007). "SSR180711, a novel selective alpha7 nicotinic receptor partial agonist: (1) binding and functional profile". Neuropsychopharmacology 32 (1): 1–16. doi:. PMID 17019409.
- ^ Macor JE, Gurley D, Lanthorn T, et al (2001). "The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist". Bioorg. Med. Chem. Lett. 11 (3): 319–21. PMID 11212100.
- ^ Whiteaker P, Christensen S, Yoshikami D, et al (2007). "Discovery, synthesis, and structure activity of a highly selective alpha7 nicotinic acetylcholine receptor antagonist". Biochemistry 46 (22): 6628–38. doi:. PMID 17497892.
- ^ Tsuneki H, You Y, Toyooka N, et al (2004). "Alkaloids indolizidine 235B', quinolizidine 1-epi-207I, and the tricyclic 205B are potent and selective noncompetitive inhibitors of nicotinic acetylcholine receptors". Mol. Pharmacol. 66 (4): 1061–9. doi:. PMID 15258256.
- ^ Grønlien JH, Håkerud M, Ween H, et al (2007). "Distinct profiles of alpha7 nAChR positive allosteric modulation revealed by structurally diverse chemotypes". Mol. Pharmacol. 72 (3): 715–24. doi:. PMID 17565004.
- ^ Hurst RS, Hajós M, Raggenbass M, et al (2005). "A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization". J. Neurosci. 25 (17): 4396–405. doi:. PMID 15858066.
- ^ Timmermann DB, Grønlien JH, Kohlhaas KL, et al (2007). "An allosteric modulator of the alpha7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo". J. Pharmacol. Exp. Ther. 323 (1): 294–307. doi:. PMID 17625074.
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