634616-95-8
634616-95-8 structure
- Name: TBPB
- Chemical Name: 1-[1'-(2-Methylbenzyl)-1,4'-bipiperidin-4-yl]-1,3-dihydro-2H-benz imidazol-2-one
- CAS Number: 634616-95-8
- Molecular Formula: C25H32N4O
- Molecular Weight: 404.548
- Catalog: Signaling Pathways GPCR/G Protein mAChR
- Create Date: 2017-10-12 15:43:39
- Modify Date: 2024-01-02 09:27:01
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TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that regulates amyloid processing and produces antipsychotic-like activity in rats.IC50 value: 289 nM(EC50) [2]Target: M1 mAChR agonistin vitro: TBPB activates M(1) through an allosteric site rather than the orthosteric acetylcholine binding site, which is likely critical for its unprecedented selectivity. Whole-cell patch-clamp recordings demonstrated that activation of M(1) by TBPB potentiates NMDA receptor currents in hippocampal pyramidal cells but does not alter excitatory or inhibitory synaptic transmission, responses thought to be mediated by M(2) and M(4) [1]. in vivo: TBPB was efficacious in models predictive of antipsychotic-like activity in rats at doses that did not produce catalepsy or peripheral adverse effects of other mAChR agonists [1].
| Name | 1-[1'-(2-Methylbenzyl)-1,4'-bipiperidin-4-yl]-1,3-dihydro-2H-benz imidazol-2-one |
|---|---|
| Synonyms |
2H-Benzimidazol-2-one, 1,3-dihydro-1-[1'-[(2-methylphenyl)methyl][1,4'-bipiperidin]-4-yl]-
2-Pyrrolo-1,3,2-dioxa-phospholan 1-[1'-(2-Methylbenzyl)-1,4'-bipiperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one 2-pyrrol-1-yl-1,3,2-dioxaphospholan TBPB |
| Description | TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that regulates amyloid processing and produces antipsychotic-like activity in rats.IC50 value: 289 nM(EC50) [2]Target: M1 mAChR agonistin vitro: TBPB activates M(1) through an allosteric site rather than the orthosteric acetylcholine binding site, which is likely critical for its unprecedented selectivity. Whole-cell patch-clamp recordings demonstrated that activation of M(1) by TBPB potentiates NMDA receptor currents in hippocampal pyramidal cells but does not alter excitatory or inhibitory synaptic transmission, responses thought to be mediated by M(2) and M(4) [1]. in vivo: TBPB was efficacious in models predictive of antipsychotic-like activity in rats at doses that did not produce catalepsy or peripheral adverse effects of other mAChR agonists [1]. |
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| Related Catalog | |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Molecular Formula | C25H32N4O |
| Molecular Weight | 404.548 |
| Exact Mass | 404.257599 |
| PSA | 44.53000 |
| LogP | 4.96 |
| Index of Refraction | 1.623 |
| Storage condition | 2-8℃ |
| RIDADR | NONH for all modes of transport |
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|
~75%
634616-95-8 |
| Literature: Rasheed, Mohammed Abdul; Shaik, Nagul Meera; Nirogi, Ramakrishna Synthetic Communications, 2013 , vol. 43, # 13 p. 1796 - 1801 |
|
~82%
634616-95-8 |
| Literature: Bridges, Thomas M.; Brady, Ashley E.; Phillip Kennedy; Nathan Daniels; Miller, Nicole R.; Kim, Kwango; Breininger, Micah L.; Gentry, Patrick R.; Brogan, John T.; Jones, Carrie K.; Jeffrey Conn; Lindsley, Craig W. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 20 p. 5439 - 5442 |
|
~%
634616-95-8 |
| Literature: Rasheed, Mohammed Abdul; Shaik, Nagul Meera; Nirogi, Ramakrishna Synthetic Communications, 2013 , vol. 43, # 13 p. 1796 - 1801 |
|
~%
634616-95-8 |
| Literature: Rasheed, Mohammed Abdul; Shaik, Nagul Meera; Nirogi, Ramakrishna Synthetic Communications, 2013 , vol. 43, # 13 p. 1796 - 1801 |
|
~%
634616-95-8 |
| Literature: Rasheed, Mohammed Abdul; Shaik, Nagul Meera; Nirogi, Ramakrishna Synthetic Communications, 2013 , vol. 43, # 13 p. 1796 - 1801 |
| Precursor 5 | |
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| DownStream 0 | |