Imbutamine
Imbutamine is a histamine H3 receptor (H3R) agonist that activates the GPCR regulating neurotransmitter release. Imbutamine binds to human H3R with a pKi of 8.4 and a Ki of 4.27 nM, activates human H3R-mediated G protein signaling with an EC50 of 3.13 nM, and exhibits near-full intrinsic agonist activity. Imbutamine is more selective for human H3R than for human H4R, activates human H4R-mediated G protein signaling with an EC50 of 66.1 nM, and binds to human H4R with a Ki of 12.7 nM.
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- CAS No.: 40546-47-2
- Formula: C7H13N3
- Molecular Weight:139.20
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histamine Receptor Isoforms
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Biological Activity
Description
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H3 Receptor 4.27 nM (Ki) |
H4 receptor 12.7 nM (Ki) |
In Vitro
Imbutamine is a full agonist at human H3R in a cAMP accumulation assay with pEC50 8.3 and α 1.0[1].
Imbutamine binds the human H3 receptor in SK-N-MC cell membranes with pKi 8.4[2].
Imbutamine binds the human H4 receptor in SK-N-MC cell membranes with pKi 7.8 and shows 3.6-fold selectivity for human H3 over human H4[2].
Imbutamine (6 h) acts as a full agonist at the human H3 receptor in SK-N-MC cells with pEC50 8.1[2].
Imbutamine (1×10-5-1×10-12 M; 5 min) shows moderate isoform bias toward hH3R-445 over hH3R-329 and favors hH3R-415 over hH3R-329 in HEK293T cells expressing hH3R isoforms in CAMYEL BRET cAMP inhibition assays[4].
Imbutamine has Ki values of 12.7 nM and 4.3 nM at recombinant human histamine H4 and H3 receptors, respectively[5].
Imbutamine is a potent agonist at Sf9 membrane-expressed hH3R (EC50 3.13 nM) and hH4R (EC50 66.1 nM), with higher potency at hH3R[6].
Imbutamine (60 min) binds hH3R with Ki 4.27 nM and hH4R with Ki 12.7 nM in Sf9 membrane preparations[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 40546-47-2
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Molecular Weight 139.20
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Formula C7H13N3
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SMILES
NCCCCC1=CN=CN1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)