spiro(1-azabicyclo(2.2.2)octane-3,2'(3H)-furo(2,3-b)pyridine): AZD-0328 is the (2'R)-isomer and D-tartrate salt; an alpha7 neuronal nicotinic receptor agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 9794392 |
| CHEMBL ID | 2151437 |
| SCHEMBL ID | 1459640 |
| MeSH ID | M0539230 |
| Synonym |
|---|
| ar-r23465xx |
| azd-0328 |
| SCHEMBL1459640 |
| spiro(1-azabicyclo(2.2.2)octane-3,2'(3h)-furo(2,3-b)pyridine) |
| 2b218x5qiy , |
| azd0328 |
| azd 0328 |
| unii-2b218x5qiy |
| spiro(1-azabicyclo(2.2.2)octane-3,2'(3'h)-furo(2,3-b)pyridine), (2'r)- |
| 220099-91-2 |
| bdbm50393243 |
| chembl2151437 , |
| azd 0328 [who-dd] |
| gtpl7697 |
| (8r)-spiro[1-azabicyclo[2.2.2]octane-8,2'-3h-furo[5,4-b]pyridine] |
| (r)-(-)-spiro[1-azabicyclo[2.2.2]octane-3,2'(3'h)-furo[2,3-b]pyridine] |
| (r)-(-)-spiro[1-azabicyclo[2.2.2]octane-3,2' (3'h)-furo[2,3-b]pyridine] |
| OCKIPDMKGPYYJS-ZDUSSCGKSA-N , |
| AKOS027324863 |
| DB12145 |
| spiro[1-azabicyclo[2.2.2]octane-3,2'(3'h)-furo[2,3-b]pyridine], (2'r)- |
| 3'h-spiro[4-azabicyclo[2.2.2]octane-2,2'-furo[2,3-b]pyridine] |
| DTXSID40944616 |
| Q17014648 |
| (2r)-3h-1'-azaspiro[furo[2,3-b]pyridine-2,3'-bicyclo[2.2.2]octane] |
| (3r)-spiro[1-azabicyclo[2.2.2]octane-3,2'-3h-furo[2,3-b]pyridine] |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Peak extracellular dopamine levels were reached 2h after dosing with AZD0328." | ( Selective alpha7 nicotinic receptor activation by AZD0328 enhances cortical dopamine release and improves learning and attentional processes. Christian, EP; Doherty, JJ; Gordon, JC; Gurley, D; Hudzik, T; Johnson, E; Jonak, G; Li, C; Maciag, C; Mrzljak, L; Piser, T; Quirk, MC; Smagin, GN; Smith, JS; Song, D; Sutton, EJ; Sydserff, S; Wang, Y; Widzowski, D, 2009) | 0.35 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Neuronal acetylcholine receptor subunit beta-2 | Homo sapiens (human) | Ki | 0.1400 | 0.0000 | 0.1117 | 3.5400 | AID690411 |
| Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) | Ki | 0.0030 | 0.0022 | 1.7427 | 10.0000 | AID1366573; AID690414 |
| Neuronal acetylcholine receptor subunit alpha-4 | Homo sapiens (human) | Ki | 0.1400 | 0.0000 | 0.1157 | 3.5400 | AID690411 |
| 5-hydroxytryptamine receptor 3A | Homo sapiens (human) | Ki | 0.0120 | 0.0000 | 0.7411 | 9.9000 | AID690410 |
| Neuronal acetylcholine receptor subunit alpha-7 | Rattus norvegicus (Norway rat) | Ki | 0.0050 | 0.0000 | 0.7307 | 8.0000 | AID1366572 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) | EC50 (µMol) | 0.3400 | 0.1280 | 2.8018 | 8.9000 | AID690413 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID690411 | Binding affinity to human alpha4beta2 nAChR | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery and development of α7 nicotinic acetylcholine receptor modulators. |
| AID730780 | Ratio of drug level in brain to plasma in sc dosed rat after 30 mins | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Discovery of a novel series of quinolone α7 nicotinic acetylcholine receptor agonists. |
| AID690413 | Agonist activity at human alpha7 nAChR | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery and development of α7 nicotinic acetylcholine receptor modulators. |
| AID690410 | Binding affinity to human 5HT3A receptor | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery and development of α7 nicotinic acetylcholine receptor modulators. |
| AID730782 | Dissociation constant, pKa of the compound | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Discovery of a novel series of quinolone α7 nicotinic acetylcholine receptor agonists. |
| AID690412 | Agonist activity at human alpha7 nAChR relative to control | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery and development of α7 nicotinic acetylcholine receptor modulators. |
| AID1366572 | Displacement of [125I]alpha-bungarotoxin from rat alpha7 nAChR expressed in HEK293 cell membranes after 2 hrs by topcount scintillation counting analysis | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | Design and synthesis of a novel series of (1'S,2R,4'S)-3H-4'-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2'-bicyclo[2.2.2]octanes] with high affinity for the α7 neuronal nicotinic receptor. |
| AID690414 | Binding affinity to human alpha7 nAchR | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery and development of α7 nicotinic acetylcholine receptor modulators. |
| AID730781 | Permeability of the compound at pH 7.4 by PAMPA | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Discovery of a novel series of quinolone α7 nicotinic acetylcholine receptor agonists. |
| AID1366573 | Displacement of [125I]alpha-bungarotoxin from human alpha7 nAChR expressed in HEK293 cell membranes after 2 hrs by topcount scintillation counting analysis | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | Design and synthesis of a novel series of (1'S,2R,4'S)-3H-4'-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2'-bicyclo[2.2.2]octanes] with high affinity for the α7 neuronal nicotinic receptor. |
| AID730779 | Efflux ratio of the compound in human Caco2 cells | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Discovery of a novel series of quinolone α7 nicotinic acetylcholine receptor agonists. |
| AID1346583 | Human nicotinic acetylcholine receptor alpha7 subunit (Nicotinic acetylcholine receptors) | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery and development of α7 nicotinic acetylcholine receptor modulators. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (14.29) | 29.6817 |
| 2010's | 6 (85.71) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (14.29%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (85.71%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||