Page last updated: 2024-11-12
crispine a
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
crispine A: pyrrolo(2,1-a)isoquinoline alkaloid from Carduus crispus; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Related Flora
| Flora | Rank | Flora Definition | Family | Family Definition |
|---|---|---|---|---|
| Carduus | genus | A plant genus of the family ASTERACEAE. Members contain arctiin and onopordopicrin.[MeSH] | Asteraceae | A large plant family of the order Asterales, subclass Asteridae, class Magnoliopsida. The family is also known as Compositae. Flower petals are joined near the base and stamens alternate with the corolla lobes. The common name of daisy refers to several genera of this family including Aster; CHRYSANTHEMUM; RUDBECKIA; TANACETUM.[MeSH] |
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 10263398 |
| CHEMBL ID | 3235509 |
| MeSH ID | M0514756 |
Synonyms (8)
| Synonym |
|---|
| inchi=1/c14h19no2/c1-16-13-8-10-5-7-15-6-3-4-12(15)11(10)9-14(13)17-2/h8-9,12h,3-7h2,1-2h |
| 8,9-dimethoxy-2,3,4,5,6,10b-hexahydro-1h-pyrrolo[2,1-a]isoquinoline |
| 8,9-DIMETHOXY-1,2,3,5,6,10B-HEXAHYDROPYRROLO[2,1-A]ISOQUINOLINE , |
| 15889-93-7 |
| 1,2,3,5,6,10b-hexahydro-8,9-dimethoxypyrrolo[2,1-a]isoquinoline |
| crispine a |
| CHEMBL3235509 , |
| bdbm50006633 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (7)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Neuronal acetylcholine receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 100.0000 | 0.0030 | 0.7770 | 6.0000 | AID1127788; AID1489907 |
| Neuronal acetylcholine receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Ki | 200.0000 | 0.0000 | 0.3522 | 10.0000 | AID1127785; AID1489903 |
| Neuronal acetylcholine receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Ki | 52.5250 | 0.0000 | 0.1234 | 5.5000 | AID1127783; AID1127784; AID1489901; AID1489902 |
| Neuronal acetylcholine receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Ki | 5.0500 | 0.0000 | 0.1082 | 5.5000 | AID1127783; AID1489901 |
| Neuronal acetylcholine receptor subunit beta-4 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 100.0000 | 0.0030 | 0.8869 | 6.0000 | AID1127788; AID1489907 |
| Neuronal acetylcholine receptor subunit beta-4 | Rattus norvegicus (Norway rat) | Ki | 150.0000 | 0.0000 | 0.2963 | 10.0000 | AID1127784; AID1127785; AID1489902; AID1489903 |
| Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0020 | 4.1527 | 9.9000 | AID1489909 |
| Neuronal acetylcholine receptor subunit beta-4 | Mus musculus (house mouse) | IC50 (µMol) | 30.5000 | 0.0040 | 0.6020 | 1.2000 | AID1127787; AID1489908 |
| Neuronal acetylcholine receptor subunit beta-2 | Mus musculus (house mouse) | IC50 (µMol) | 30.5000 | 0.0040 | 0.6020 | 1.2000 | AID1127787; AID1489908 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) | EC50 (µMol) | 100.0000 | 0.1280 | 2.8018 | 8.9000 | AID1489910 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (38)
Molecular Functions (10)
Ceullar Components (8)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) |
| membrane | Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) |
| plasma membrane raft | Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) |
| postsynaptic membrane | Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) |
| postsynapse | Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) |
| acetylcholine-gated channel complex | Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) |
| plasma membrane | Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) |
| neuron projection | Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) |
| synapse | Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Bioassays (13)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1489903 | Displacement of [3H]epibatidine from rat alpha3beta4 nAChR expressed in HEK293 cell membranes after 4 hrs by scintillation counting method | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts. |
| AID1489909 | Antagonist activity at human alpha7 nAChR expressed in HEK293 cells co-expressing Ric-3/NACHO assessed as inhibition of ACh-induced calcium mobilization measured up to 90 secs in presence of PNU-120596 by FLIPR assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts. |
| AID1127783 | Displacement of [3H]epibatidine from rat alpha4/beta2 nAChR expressed in HEK293 cells | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | Design, synthesis, and biological evaluation of Erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists. |
| AID1127784 | Displacement of [3H]epibatidine from rat alpha4/beta4 nAChR expressed in HEK293 cells | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | Design, synthesis, and biological evaluation of Erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists. |
| AID1127787 | Antagonist activity at mouse alpha4/beta2 nAChR expressed in HEK293 cells assessed as inhibition of (S)-nicotine-induced activity by FLIPR membrane potential blue assay | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | Design, synthesis, and biological evaluation of Erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists. |
| AID1127788 | Antagonist activity at rat alpha3/beta4 nAChR expressed in HEK293 cells assessed as inhibition of (S)-nicotine-induced activity by FLIPR membrane potential blue assay | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | Design, synthesis, and biological evaluation of Erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists. |
| AID1489908 | Antagonist activity at mouse alpha4beta2 nAChR expressed in HEK293 cells assessed as inhibition of (S)-nicotine-induced current response measured up to 90 secs by FMP assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts. |
| AID1489910 | Agonist activity at human alpha7 nAChR expressed in HEK293 cells co-expressing Ric-3/NACHO assessed as induction of calcium mobilization measured up to 90 secs in presence of PNU-120596 by FLIPR assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts. |
| AID1489902 | Displacement of [3H]epibatidine from rat alpha4beta4 nAChR expressed in HEK293 cell membranes after 4 hrs by scintillation counting method | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts. |
| AID1127785 | Displacement of [3H]epibatidine from rat alpha3/beta4 nAChR expressed in HEK293 cells | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | Design, synthesis, and biological evaluation of Erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists. |
| AID1127786 | Displacement of [3H]MLA from rat/mouse alpha7 nAChR/5HT3A expressed in tsA201 cells | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | Design, synthesis, and biological evaluation of Erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists. |
| AID1489901 | Displacement of [3H]epibatidine from rat alpha4beta2 nAChR expressed in HEK293 cell membranes after 4 hrs by scintillation counting method | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts. |
| AID1489907 | Antagonist activity at rat alpha3beta4 nAChR expressed in HEK293 cells assessed as inhibition of (S)-nicotine-induced current response measured up to 90 secs by FMP assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (13)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (23.08) | 29.6817 |
| 2010's | 10 (76.92) | 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] | ||
Market Indicators
Research Demand Index: 17.33
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (17.33) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 13 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||