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B-HT 933 dihydrochloride
- Azepexole
- Parent CAS: 36067-73-9
- Soluble in water and DMSO
- MF: C9H15N3O.2HCl
- MW: 254.16
Description
B-HT 933 dihydrochloride (Azepexole) is a potent and selective α2-adrenoceptor agonist. It binds with high affinity to α2A, α2B, and α2C subtypes with pKi of 8.3, 7.6 and 7.5, respectively. It exhibits greater than 300-fold selectivity for α2-adrenoceptor over the α1-adrenoceptor. In pharmacological and functional assays, it demonstrates an IC50 value of 78.72 nM for the inhibition of peristaltic contractions in tissue preparations. It is widely used to activate α2-adrenergic signaling in studies of presynaptic neurotransmitter release, sympathetic regulation and CNS adrenergic pathways.
α2-Adrenoceptors are Gi/o-coupled receptors that regulate norepinephrine release, autonomic tone and neuronal excitability. B-HT 933 dihydrochloride provides a selective agonist tool for adrenergic receptor pharmacology.
Key Features
- Selective α2-adrenoceptor agonist
- Activates Gi/o-coupled adrenergic signaling
- Useful for presynaptic autoreceptor studies
- Modulates α2-adrenoceptor signaling
Applications
- α2-Adrenoceptor pharmacology
- Adrenergic neurotransmission research
- Autonomic signaling studies
- Presynaptic release modulation assays
More Information
| Parent CAS No. | 36067-73-9 |
|---|---|
| Chemical Name | 6-Ethyl-5,6,7,8-tetrahydro-4H-oxazolo[4,5-d]azepin-2-ylamine dihydrochloride |
| SMILES | C12N=C(OC=1CCN(CC)CC2)N.Cl.Cl |
| MFCD | MFCD01529923 |
| InChi | InChI=1S/C9H15N3O.2ClH/c1-2-12-5-3-7-8(4-6-12)13-9(10)11-7;;/h2-6H2,1H3,(H2,10,11);2*1H |
| InChiKey | HBLPYIOKPJVFQW-UHFFFAOYSA-N |
| CID | 169743 |
| Short Description | α2 agonist |
References
- Browne et al. Differential patterns of local cerebral glucose utilisation associated with rilmenidine- or B-HT 933-induced hypotension. Brain Res. 1994, 666, 216-222.
- H. Nielson et al. Calcium utilization coupled to stimulation of post junctional alpha-1 and alpha-2 adrenoceptors in isolated human resistance arteries. J. Pharmacol. Exp. Ther. 1992, 260, 637-643.
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