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B-HT 933 dihydrochloride

α2-adrenoceptor agonist CAS# 36067-72-8

B-HT 933 dihydrochloride

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Chemical structure

B-HT 933 dihydrochloride

3D structure

Chemical Properties of B-HT 933 dihydrochloride

Cas No. 36067-72-8 SDF Download SDF
PubChem ID 169743 Appearance Powder
Formula C9H17Cl2N3O M.Wt 254.16
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Azepexole
Solubility Soluble to 100 mM in water and to 100 mM in DMSO
Chemical Name 6-ethyl-4,5,7,8-tetrahydro-[1,3]oxazolo[4,5-d]azepin-2-amine;dihydrochloride
SMILES CCN1CCC2=C(CC1)OC(=N2)N.Cl.Cl
Standard InChIKey HBLPYIOKPJVFQW-UHFFFAOYSA-N
Standard 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of B-HT 933 dihydrochloride

DescriptionSelective α2-adrenoceptor agonist. Exhibits greater than 300-fold selectivity for the α2-adrenoceptor over the α1-adrenoceptor.

B-HT 933 dihydrochloride Dilution Calculator

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B-HT 933 dihydrochloride Molarity Calculator

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Preparing Stock Solutions of B-HT 933 dihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.9345 mL 19.6726 mL 39.3453 mL 78.6906 mL 98.3632 mL
5 mM 0.7869 mL 3.9345 mL 7.8691 mL 15.7381 mL 19.6726 mL
10 mM 0.3935 mL 1.9673 mL 3.9345 mL 7.8691 mL 9.8363 mL
50 mM 0.0787 mL 0.3935 mL 0.7869 mL 1.5738 mL 1.9673 mL
100 mM 0.0393 mL 0.1967 mL 0.3935 mL 0.7869 mL 0.9836 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on B-HT 933 dihydrochloride

IC50: 0.44 μM

The contractile effects of adrenaline and noradrenaline may be mediated by both postjunctional α2- and α2-adrenoceptors on vascular smooth muscle. B-HT 933 is a selective α2-adrenoceptor agonist.

In vitro: B-HT 933, a selective α2-adrenoceptor agonist, contracts human subcutaneous resistance arteries by a mechanism largely dependent on the influx of extracellular Ca2+, probably through voltage-operated calcium channels. This action involves a pertussis toxin-sensitive G protein, possibly GQ [1].

In vivo: The dose-related effects of the selective α2-adrenoceptor agonist B-HT 933 on the body temperature of untreated and reserpine-treated mice were investigated. In untreated mice B-HT 933 induced a dose-related hypothermia. The highest dose of B-HT 933 elicited a marked hypothermia, whereas the maximal hypothermic effect of clonidine was less pronounced and reached a plateau at a dose of 0.5 mg/kg [2].

Clinical trial: Up to now, B-HT 933 is still in the preclinical development stage.

Reference:
[1] N. A. Parkinson & A.D. Hughes. The mechanism of action of 1c2-adrenoceptors in human isolated subcutaneous resistance arteries. British Journal of Pharmacology (1995) 115, 1463-1468
[2] D. J. Bill, I.E. Hughes & R.J. Stephens. The thermogenic actions of x2-adrenoceptor agonists in reserpinized mice are mediated via a central postsynaptic ac2-adrenoceptor mechanism. Br. J. Pharmacol. (1989), 96, 133-143

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References on B-HT 933 dihydrochloride

The mechanism of action of alpha 2-adrenoceptors in human isolated subcutaneous resistance arteries.[Pubmed:8564206]

Br J Pharmacol. 1995 Aug;115(8):1463-8.

1. The effect of noradrenaline and the selective alpha 2-adrenoceptor agonist, azepexole, on tone and intracellular Ca2+ ([Ca2+]i) was examined in human isolated subcutaneous resistance arteries. Isolated arteries were mounted on an isometric myograph and loaded with the Ca2+ indicator, fura-2, for simultaneous measurement of force and [Ca2+]i. 2. High potassium solution (KPSS), noradrenaline and azepexole increased [Ca2+]i and contracted subcutaneous arteries in physiological saline. When extracellular Ca2+ was removed and the calcium chelator, BAPTA, added to the physiological saline (PSSo), responses to noradrenaline were transient and reduced, and responses to azepexole were markedly inhibited. 3. Ryanodine, an agent which interferes with Ca2+ release from intracellular stores, had little effect on contractile responses to KPSS, noradrenaline or azepexole in physiological saline. The response to caffeine in physiological saline was inhibited by ryanodine. In PSSo, ryanodine partially inhibited contractile responses to noradrenaline and azepexole, and completely abolished the response to caffeine. 4. Noradrenaline and azepexole both significantly increased maximum force achieved by cumulative addition of Ca2+ to a Ca(2+)-free depolarizing solution and shifted the calculated relationship between [Ca2+]i and force to the left, suggesting these agents increase the sensitivity of the contractile apparatus to [Ca2+]i. 5. (-)-202 791, a dihydropyridine antagonist of voltage-operated calcium channels partially inhibited both the contractile response and the rise in [Ca2+]i induced by azepexole. Pre-treatment of arteries with pertussis toxin inhibited responses to azepexole, but had no significant effect on tone induced by KPSS or noradrenaline. ETYA, an inhibitor of phospholipase A2, lipoxygenase and cyclo-oxygenase, had no effect on azepexole-induced contraction in the presence of N omega nitro-L-arginine methyl ester.6. Azepexole, a selective alpha2-adrenoceptor agonist, contracts human subcutaneous resistance arteries by a mechanism largely dependent on the influx of extracellular Ca2", probably through voltage-operated calcium channels. This action involves a pertussis toxin-sensitive G protein, possibly Gi.

The thermogenic actions of alpha 2-adrenoceptor agonists in reserpinized mice are mediated via a central postsynaptic alpha 2-adrenoceptor mechanism.[Pubmed:2564288]

Br J Pharmacol. 1989 Jan;96(1):133-43.

1. The dose-related effects of the selective alpha 2-adrenoceptor agonists clonidine, UK-14,304 and B-HT 933 on the body temperature of untreated and reserpine-treated mice were investigated. 2. In untreated mice all three agonists induced a dose-related hypothermia. The highest doses of UK-14,304 and B-HT 933, 3 and 100 mg kg-1 respectively, elicited a marked (10 degrees C) hypothermia, whereas the maximal hypothermic effect of clonidine (5.5 degrees C) was less pronounced and reached a plateau at a dose of 0.5 mg kg-1 i.p. 3. Reserpine (2.5 mg kg-1, s.c.) induced a marked hypothermia in the mouse; 18 h after injection body temperature had decreased to only slightly (0.5-1.5 degrees C) above ambient (19 degrees C). 4. All three alpha 2-agonists produced a partial dose-related reversal of reserpine-induced hypothermia; maximal thermogenic responses (9-10 degrees C increases in body temperature) were elicited by doses of 0.2, 0.5 and 16 mg kg-1 i.p. of clonidine, UK-14,304 and B-HT 933 respectively, and the log dose-response curves for all 3 agonists were bell-shaped. 5. Following intracerebroventricular administration to reserpine-treated mice, the thermogenic response to clonidine was more rapid in onset, and the agonist was 20 fold more potent than when injected i.p. 6. The selective alpha 2-adrenoceptor antagonists, idazoxan (0.05-0.5 mg kg-1), Wy 26392 (0.3-5.0 mg kg-1) and yohimbine (0.1-1.6 mg kg-1) given orally attenuated the thermogenic responses to all 3 agonists in reserpinized mice in a dose-related manner. Pretreatment with a single dose of idazoxan (0.3 mg kg-1, orally) elicited a 6 fold parallel shift to the right in the dose-response curve to clonidine. 7. The selective alpha 1-adrenoceptor antagonists, prazosin (10 mg kg-1) and indoramin (3-10 mg kg-1), and the beta-adrenoceptor antagonist, propranolol (10 mg kg-1), only partially attenuated the thermogenic responses to the alpha 2-agonists in reserpinized mice. These effects were variable and not clearly dose-related. 8. Pretreatment of reserpinized mice with the catecholamine synthesis inhibitor, alpha-methyl-p-tyrosine, markedly attenuated (60-95%) the thermogenic response to the noradrenaline uptake inhibitor, desipramine (0.13-12.5 mg kg-1, i.p.), but only slightly reduced (10-35%) that to clonidine (0.032-0.5 mg kg-1, i.p.). 9. These results suggest that alpha2-adrenoceptor agonists reverse reserpine-induced hypothermia via a central mechanism involving activation of postsynaptic alpha 2-adrenoceptors.

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