From Wikipedia, the free encyclopedia
Pharmaceutical drug
Sazetidine A (AMOP-H-OH) is a drug which acts as a subtype selective partial agonist at α4β2 neural nicotinic acetylcholine receptors, acting as an agonist at (α4)2(β2)3 pentamers, but as an antagonist at (α4)3(β2)2 pentamers.[1][2] It has potent analgesic effects in animal studies comparable to those of epibatidine, but with less toxicity,[3] and also has antidepressant action.[4]
- ^ Xiao Y, Fan H, Musachio JL, Wei ZL, Chellappan SK, Kozikowski AP, Kellar KJ (October 2006). "Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them". Molecular Pharmacology. 70 (4): 1454–60. doi:10.1124/mol.106.027318. PMID 16857741. S2CID 6599272.
- ^ Zwart R, Carbone AL, Moroni M, Bermudez I, Mogg AJ, Folly EA, et al. (June 2008). "Sazetidine-A is a potent and selective agonist at native and recombinant alpha 4 beta 2 nicotinic acetylcholine receptors". Molecular Pharmacology. 73 (6): 1838–43. doi:10.1124/mol.108.045104. PMID 18367540. S2CID 24632914.
- ^ Cucchiaro G, Xiao Y, Gonzalez-Sulser A, Kellar KJ (September 2008). "Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug". Anesthesiology. 109 (3): 512–9. doi:10.1097/ALN.0b013e3181834490. PMID 18719450. S2CID 22185882.
- ^ Kozikowski AP, Eaton JB, Bajjuri KM, Chellappan SK, Chen Y, Karadi S, et al. (August 2009). "Chemistry and pharmacology of nicotinic ligands based on 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol (AMOP-H-OH) for possible use in depression". ChemMedChem. 4 (8): 1279–91. doi:10.1002/cmdc.200900079. PMC 2955514. PMID 19569163.
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SSRIsTooltip Selective serotonin reuptake inhibitors | |
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SNRIsTooltip Serotonin–norepinephrine reuptake inhibitors | |
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NRIsTooltip Norepinephrine reuptake inhibitors | |
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NDRIsTooltip Norepinephrine–dopamine reuptake inhibitors | |
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NaSSAsTooltip Noradrenergic and specific serotonergic antidepressants | |
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SARIsTooltip Serotonin antagonist and reuptake inhibitors | |
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SMSTooltip Serotonin modulator and stimulators | |
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Others | |
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TCAsTooltip Tricyclic antidepressants | |
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TeCAsTooltip Tetracyclic antidepressants | |
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Others | |
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Non-selective | |
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MAOATooltip Monoamine oxidase A-selective | |
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MAOBTooltip Monoamine oxidase B-selective | |
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nAChRsTooltip Nicotinic acetylcholine receptors | Agonists (and PAMsTooltip positive allosteric modulators) |
- 5-HIAA
- 6-Chloronicotine
- A-84,543
- A-366,833
- A-582,941
- A-867,744
- ABT-202
- ABT-418
- ABT-560
- ABT-894
- Acetylcholine
- Altinicline
- Anabasine
- Anatabine
- Anatoxin-a
- AR-R17779
- Bephenium hydroxynaphthoate
- Butinoline
- Butyrylcholine
- Carbachol
- Choline
- Cotinine
- Cytisine
- Decamethonium
- Desformylflustrabromine
- Dianicline
- Dimethylphenylpiperazinium
- Epibatidine
- Epiboxidine
- Ethanol (alcohol)
- Ethoxysebacylcholine
- EVP-4473
- EVP-6124
- Galantamine
- GTS-21
- Ispronicline
- Ivermectin
- JNJ-39393406
- Levamisole
- Lobeline
- MEM-63,908 (RG-3487)
- Morantel
- Nicotine (tobacco)
- NS-1738
- PHA-543,613
- PHA-709,829
- PNU-120,596
- PNU-282,987
- Pozanicline
- Pyrantel
- Rivanicline
- RJR-2429
- Sazetidine A
- SB-206553
- Sebacylcholine
- SIB-1508Y
- SIB-1553A
- SSR-180,711
- Suberyldicholine
- Suxamethonium (succinylcholine)
- Suxethonium (succinyldicholine)
- TC-1698
- TC-1734
- TC-1827
- TC-2216
- TC-5214
- TC-5619
- TC-6683
- Tebanicline
- Tribendimidine
- Tropisetron
- UB-165
- Varenicline
- WAY-317,538
- XY-4083
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Antagonists (and NAMsTooltip negative allosteric modulators) | |
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Precursors (and prodrugs) | |
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