HEAT hydrochloride
Names
[ CAS No. ]:
30007-39-7
[ Name ]:
HEAT hydrochloride
[Synonym ]:
HEAT
HEAT hydrochloride
BE-2254 hydrochloride
Biological Activity
[Description]:
HEAT (BE2254) hydrochloride is a selective alpha 1 adrenergic receptor antagonist. HEAT hydrochloride, a phenethylamine derivative, shows pKis of 9, 9.1, and 8.57 for alpha 1a, alpha 1b and alpha 1c, respectively[1][2].
[Related Catalog]:
[In Vitro]
BE2254 inhibits (-)-noradrenaline-mediated increases in gluconeogenesis with K,sub>B of 0.74 nM[2]. The alpha-1 selective antagonist [125I]BE2254 is used to specifically label a single class of binding sites with a dissociation constant of 131.0 pM and a maximal binding capacity of 17.6 fmol/mg of protein. Catecholamines compete for [125I]BE2254 binding stereospecifically and with the characteristic alpha adrenergic potency series of (-)-epinephrine greater than (-)-norepinephrine much greater than (-)-isoproterenol. The alpha-1 selective antagonist prazosin (Kd=2.4 nM) is much more potent in competing for [125I]BE2254 binding than is the alpha-2 selective antagonist yohimbine (Kd=2900 nM)[3].
[References]
Chemical & Physical Properties
[ Boiling Point ]:
492.8ºC at 760mmHg
[ Molecular Formula ]:
C19H22ClNO2
[ Molecular Weight ]:
331.83600
[ Flash Point ]:
251.9ºC
[ Exact Mass ]:
331.13400
[ PSA ]:
49.33000
[ LogP ]:
4.16250
Toxicological Information
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- QK4750000
- CHEMICAL NAME :
- 1(2H)-Naphthalenone, 3,4-dihydro-2-(((2-p-hydroxyphenyl)ethylamino)methyl) -, hydrochloride
- CAS REGISTRY NUMBER :
- 30007-39-7
- LAST UPDATED :
- 199706
- DATA ITEMS CITED :
- 4
- MOLECULAR FORMULA :
- C19-H21-N-O2.Cl-H
- MOLECULAR WEIGHT :
- 331.87
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 650 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,231,1982
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 22500 ug/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,231,1982
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 730 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,231,1982
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 33 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,231,1982