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ABT 102
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C21H24N4O
- MW: 348.44
Description
ABT 102 is a potent and selective antagonist of the transient receptor potential vanilloid 1 (TRPV1) channel, with reported IC50 values of approximately 5–7 nM. It inhibits TRPV1 activation by noxious heat, protons and vanilloid agonists such as capsaicin.
TRPV1 integrates chemical and thermal pain signals in sensory neurons. ABT 102 is therefore useful for investigating nociceptor excitability, inflammatory hyperalgesia, thermoregulation and the pharmacology of analgesic TRPV1 blockade.
Key Features
- Potent and selective TRPV1 channel antagonist
- Reported IC50: approximately 5–7 nM
- Blocks capsaicin-, proton- and heat-evoked TRPV1 activation
- Useful for studying pain signaling and thermosensory effects
Applications
- TRPV1 ion-channel pharmacology
- Nociception and inflammatory pain models
- Capsaicin-response and sensory-neuron assays
- Thermoregulation and analgesic mechanism studies
More Information
| Parent CAS No. | 808756-71-0 |
|---|---|
| Chemical Name | (R)-1-(5-tert-Butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea |
| SMILES | C1C(NC(N[C@@H]2CCC3C=C(C(C)(C)C)C=CC2=3)=O)=C2C=NNC2=CC=1 |&1:5,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C21H24N4O/c1-21(2,3)14-8-9-15-13(11-14)7-10-18(15)24-20(26)23-17-5-4-6-19-16(17)12-22-25-19/h4-6,8-9,11-12,18H,7,10H2,1-3H3,(H,22,25)(H2,23,24,26)/t18-/m1/s1 |
| InChiKey | TYOYXJNGINZFET-GOSISDBHSA-N |
| CID | 11256560 |
| Short Description | TRPV1 antagonist |
References
- CS Surowy et al. ABT-102 Blocks Polymodal Activation of Transient Receptor Potential Vanilloid 1 Receptors in Vitro and Heat-Evoked Firing of Spinal Dorsal Horn Neurons in Vivo. JPET 2008, 326(3), 879-888.
- P Honore et al. Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia. Pain. 2009, 142(1-2), 27-35.
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