An allosteric agonist of M1 receptors
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TBPB

Item No. 22943

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,3-dihydro-1-[1'-[(2-methylphenyl)methyl][1,4'-bipiperidin]-4-yl]-2H-benzimidazol-2-one
CAS Number
634616-95-8
Molecular Formula
C25H32N4O
Formula Weight
404.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
Chloroform: 30 mg/mlDMF: 10 mg/mlDMF:PBS (pH 7.2) (1:3): 0.25 mg/ml
SMILES
CC(C=CC=C1)=C1CN(CC2)CCC2N3CCC(N4C(NC5=C4C=CC=C5)=O)CC3
InChi Code
InChI=1S/C25H32N4O/c1-19-6-2-3-7-20(19)18-27-14-10-21(11-15-27)28-16-12-22(13-17-28)29-24-9-5-4-8-23(24)26-25(29)30/h2-9,21-22H,10-18H2,1H3,(H,26,30)
InChi Key
CWPKTBMRVATCBL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $120

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    10 mg

    $180

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    Product Description

    TBPB is an allosteric agonist of M1 muscarinic acetylcholine receptors (mAChRs; EC50 = 158 nM in CHO-K1 cells expressing rat recombinant receptors).1 It is selective for M1 over M2-5 receptors at concentrations up to 10 μM. TBPB (3 μM) potentiates NMDA-evoked currents in CA1 pyramidal cells. It increases production of the non-amyloidogenic amyloid precursor protein (APP) cleavage products APPsα and CTFα in PC12 cells overexpressing the human M1 receptor and APP when used at a concentration of 1 μM. TBPB decreases amphetamine-induced hyperlocomotion in a rat model that is predictive of antipsychotic-like activity.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jones, C.K., Brady, A.E., Davis, A.A., et al. Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats. J. Neurosci. 28(41), 10422-10433 (2008).