| Name | VU0152100 |
| Description | VU0152100 is an effective and selective allosteric potentiator of M4 mAChR (EC50: 380 ± 93 nM). |
| In vitro | VU0152100 was selective for M4 relative to M1, M2, M3, and M5. VU0152100 dose-dependently potentiated the response to an EC20 concentration of ACh (EC50: 1.9 ± 0.2 μM) and increased the maximal response to ACh to approximately 130%. VU0152100 (10 μM) also increased the potency of ACh to induce GIRK-mediated thallium flux, as manifest by a robust (≈30-fold) leftward shift in the ACh CRC from 77 ± 1.2 nM (veh) to 2.35 ± 0.5 nM [1]. |
| In vivo | Systemic administration of VU0152099 and VU0152100 provides robust brain levels of these compounds, the effects of VU0152099 and VU0152100 were evaluated in reversing amphetamine-induced hyperlocomotion in rats using a dose of 56.6 mg/kg i.p. for each compound with a 30-min pretreatment interval [1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.86 mM), Sonication is recommended.
DMSO : 55 mg/mL (161.09 mM), Sonication is recommended.
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| Keywords | VU-152100 | VU-0152100 | VU0152100 | VU 152100 | VU 0152100 | Muscarinic acetylcholine receptor | mAChR | M4 mAChR | Inhibitor | inhibit |
| Inhibitors Related | Adiphenine hydrochloride | Levamisole hydrochloride | Ethyl (triphenylphosphoranylidene) acetate | Urethane | Hexamethonium Bromide | Ribavirin | Adenine | Mitotane | Choline chloride | Propoxur | N,N-Dicyclohexylcarbodiimide | Arecoline |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Neuronal Signaling Compound Library | Anti-Alzheimer's Disease Compound Library | Membrane Protein-targeted Compound Library | Anti-Parkinson's Disease Compound Library | Neurotransmitter Receptor Compound Library | NO PAINS Compound Library | Bioactive Compounds Library Max |
United States
