phenethylcymserine: structure in first source [MeSH]
| ID Source | ID |
|---|---|
| PubMed CID | 9804733 |
| CHEMBL ID | 1080386 |
| MeSH ID | M0578866 |
| Synonym |
|---|
| bdbm50312803 |
| 3alpha,8-dimethyl-1-phenethyl-1,2,3,3alpha,8,8alpha-hexahydropyrrolo[2,3-b]indol-5-yl 4-isopropylphenylcarbamate |
| (3as,8ar)-3a,8-dimethyl-1-phenethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl 4-isopropylphenylcarbamate |
| phenethylcymserine |
| CHEMBL1080386 , |
| [(3ar,8bs)-4,8b-dimethyl-3-(2-phenylethyl)-2,3a-dihydro-1h-pyrrolo[2,3-b]indol-7-yl] n-(4-propan-2-ylphenyl)carbamate |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| Cholinesterase | Homo sapiens (human) | IC50 | 0.0060 | AID1916836 |
| Acetylcholinesterase | Mus musculus (house mouse) | IC50 | 100.0000 | AID464986; AID465031 |
| Acetylcholinesterase | Homo sapiens (human) | IC50 | 22.5015 | AID1916835; AID600978; AID600980 |
| Cholinesterase | Mus musculus (house mouse) | IC50 | 0.5400 | AID464987; AID465032 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID600981 | Inhibition of human plasma BChE | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 ISSN: 1768-3254 | Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease. |
| AID600980 | Inhibition of human erythrocytes BChE | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 ISSN: 1768-3254 | Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease. |
| AID1916835 | Inhibition of AChE (unknown origin) | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240ISSN: 1768-3254 | Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease. |
| AID464988 | Selectivity ratio of IC50 for mouse serum BChE over IC50 for mouse brain AChE | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 ISSN: 1464-3405 | Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors. |
| AID1470884 | In-vivo inhibition of BuChE in Harlan-Wistar rat brain assessed as increase in acetylcholine level at 1.25 mg/kg, ip by microdialysis method relative to control | 2017 | European journal of medicinal chemistry, May-26, Volume: 132ISSN: 1768-3254 | Recent progress in the identification of selective butyrylcholinesterase inhibitors for Alzheimer's disease. |
| AID465033 | Selectivity ratio of IC50 for mouse serum BChE over IC50 for mouse brain AChE | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 ISSN: 1464-3405 | Design, synthesis and evaluation of carbamate-modified (-)-N(1)-phenethylnorphysostigmine derivatives as selective butyrylcholinesterase inhibitors. |
| AID600979 | Inhibition of human plasma AChE | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 ISSN: 1768-3254 | Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease. |
| AID1916838 | Selectivity index, ratio of IC50 for AChE (unknown origin) to BChE (unknown origin) | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240ISSN: 1768-3254 | Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease. |
| AID1470885 | In-vivo inhibition of BuChE in Harlan-Wistar rat brain assessed as increase in acetylcholine level at 2.5 mg/kg, ip by microdialysis method relative to control | 2017 | European journal of medicinal chemistry, May-26, Volume: 132ISSN: 1768-3254 | Recent progress in the identification of selective butyrylcholinesterase inhibitors for Alzheimer's disease. |
| AID465032 | Inhibition of mouse serum BChE after 1 hr by modified Ellman's colorimetric method | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 ISSN: 1464-3405 | Design, synthesis and evaluation of carbamate-modified (-)-N(1)-phenethylnorphysostigmine derivatives as selective butyrylcholinesterase inhibitors. |
| AID464987 | Inhibition of mouse serum BChE after 1 hr by modified Ellman's colorimetric method | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 ISSN: 1464-3405 | Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors. |
| AID464986 | Inhibition of mouse brain AChE after 1 hr by modified Ellman's colorimetric method | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 ISSN: 1464-3405 | Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors. |
| AID600978 | Inhibition of human erythrocytes AChE | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 ISSN: 1768-3254 | Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease. |
| AID1916836 | Inhibition of BChE (unknown origin) | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240ISSN: 1768-3254 | Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease. |
| AID465031 | Inhibition of mouse brain AChE after 1 hr by modified Ellman's colorimetric method | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 ISSN: 1464-3405 | Design, synthesis and evaluation of carbamate-modified (-)-N(1)-phenethylnorphysostigmine derivatives as selective butyrylcholinesterase inhibitors. |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 6 (85.71) | 24.3611 |
| 2020's | 1 (14.29) | 2.80 |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (28.57%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (71.43%) | 84.16% |
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| physostigmine | carbamate ester; indole alkaloid | antidote to curare poisoning; EC 3.1.1.8 (cholinesterase) inhibitor; miotic | 2012 | 2013 | 11.5 | low | 0 | 0 | 0 | 0 | 2 | 0 | |
| rivastigmine | carbamate ester; tertiary amino compound | cholinergic drug; EC 3.1.1.8 (cholinesterase) inhibitor; neuroprotective agent | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| phenserine | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |||
| tolserine | 2013 | 2013 | 11.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Acute Confusional Senile Dementia | 0 | 2011 | 2022 | 7.3 | medium | 0 | 0 | 0 | 0 | 2 | 1 | |
| Alloxan Diabetes | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Alzheimer Disease | 0 | 2011 | 2022 | 7.3 | medium | 0 | 0 | 0 | 0 | 2 | 1 | |
| Asymmetric Diabetic Proximal Motor Neuropathy | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Autoimmune Diabetes | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Diabetes Mellitus, Type 1 | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Diabetic Neuropathies | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Hyperglycemia | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Hyperglycemia, Postprandial | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Muscle Weakness | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Muscular Weakness | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Neuromuscular Junction Diseases | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |