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  • Product Name: B-HT 920
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36085-73-1

36085-73-1 structure
36085-73-1 structure
  • Name: B-HT 920
  • Chemical Name: 6-prop-2-enyl-4,5,7,8-tetrahydro-[1,3]thiazolo[4,5-d]azepin-2-amine,dihydrochloride
  • CAS Number: 36085-73-1
  • Molecular Formula: C10H17Cl2N3S
  • Molecular Weight: 282.233
  • Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
  • Create Date: 2018-03-14 08:00:00
  • Modify Date: 2024-01-09 06:21:53
  • B-HT 920(Talipexole 2Hcl) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.IC50 Value: 25 nM(Adrenergic receptor α-2, rat)Target: Adrenergic Receptor; 5-HT Receptor; Dopamine Receptorin vitro: N/Ain vivo: Intravenous injection of 30 micrograms/kg of B-HT 920 into cats lead initially to an increase in blood pressure and then to a long-lasting decrease in blood pressure and heart rate. Vagally mediated reflex bradycardia elicited by angiotensin injection in beta-adrenoceptor-blocked dogs was facilitated by intracisternal injection of 10 micrograms/kg B-HT 920.
Name 6-prop-2-enyl-4,5,7,8-tetrahydro-[1,3]thiazolo[4,5-d]azepin-2-amine,dihydrochloride
Synonyms B-HT 920 dihydrochloride
4H-Thiazolo[4,5-d]azepin-2-amine, 5,6,7,8-tetrahydro-6-(2-propen-1-yl)-, hydrochloride (1:2)
Talipexoledihydrochloride
Domin
Talipexole
5,6,7,8-Tetrahydro-6-(2-propenyl)-4H-thiazolo[4,5-d]azepine-2-amine dihydrochloride
6-Allyl-5,6,7,8-tetrahydro-4H-[1,3]thiazolo[4,5-d]azepin-2-amine dihydrochloride
B-HT 920
MFCD00274573
Description B-HT 920(Talipexole 2Hcl) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.IC50 Value: 25 nM(Adrenergic receptor α-2, rat)Target: Adrenergic Receptor; 5-HT Receptor; Dopamine Receptorin vitro: N/Ain vivo: Intravenous injection of 30 micrograms/kg of B-HT 920 into cats lead initially to an increase in blood pressure and then to a long-lasting decrease in blood pressure and heart rate. Vagally mediated reflex bradycardia elicited by angiotensin injection in beta-adrenoceptor-blocked dogs was facilitated by intracisternal injection of 10 micrograms/kg B-HT 920.
Related Catalog
References

[1]. Ricci and Taira Adrenoceptor involvement in the cardiovascular responses to B-HT 920 in sinoaortic denervated rats. Gen.Pharmacol. (1999)32 29.

[2]. Eur J Pharmacol. 1997 May 1;325(2-3):137-44.

[3]. Kohno Y, Fukuzaki K, Kitahara K, Koja T.Anti-tremor activity of talipexole produced by selective dopamine D2 receptor stimulation in cynomolgus monkeys with unilateral lesions in the ventromedial tegmentum.Eur J Pharmacol. 1997 Jan 29;319(2-3):197-205.

[4]. Momiyama T, Sasa M, Takaori S.Inhibition by talipexole, a thiazolo-azepine derivative, of dopaminergic neurons in the ventral tegmental area.Life Sci. 1991;49(7):535-43.

[5]. Nishikawa T, Yamada S, Tsuda A, Tanaka M, Koga I, Uchida Y.Chronic treatment with talipexole dihydrochloride on abnormal involuntary movement in humans.Clin Neuropharmacol. 1990 Jun;13(3):259-63.

[6]. Robertson, G.S., et al., In vivo comparisons of the effects of quinpirole and the putative presynaptic dopaminergic agonists B-HT 920 and SND 919 on striatal dopamine and acetylcholine release. J Pharmacol Exp Ther, 1993. 264(3): p. 1344-51.
Boiling Point 364.6ºC at 760mmHg
Melting Point 245ºC dec.
Molecular Formula C10H17Cl2N3S
Molecular Weight 282.233
Flash Point 174.3ºC
Exact Mass 281.052032
PSA 70.39000
LogP 3.43500

CHEMICAL IDENTIFICATION

RTECS NUMBER :
XJ7050340
CHEMICAL NAME :
4H-Thiazolo(4,5-d)azepin-2-amine, 5,6,7,8-tetrahydro-6-(2-propenyl)-, dihydrochloride
CAS REGISTRY NUMBER :
36085-73-1
LAST UPDATED :
199712
DATA ITEMS CITED :
10
MOLECULAR FORMULA :
C10-H15-N3-S.2Cl-H
MOLECULAR WEIGHT :
282.26

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 :
403 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - chromodacryorrhea Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - tremor
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,383,1993
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
66 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,383,1993
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
455 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
GWXXBX German Offenlegungsschrift Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2820808
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
>32 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Behavioral - coma
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,401,1993 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
91 mg/kg/13W-I
TOXIC EFFECTS :
Endocrine - changes in adrenal weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Reproductive - Effects on Newborn - stillbirth
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,383,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
364 mg/kg/52W-I
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - changes in lung weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Related to Chronic Data - changes in prostate weight
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,383,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
728 mg/kg/52W-I
TOXIC EFFECTS :
Blood - other changes
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 45,545,1993 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
5600 ug/kg
SEX/DURATION :
female 14 day(s) pre-mating - 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,9,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
3300 ug/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,9,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
42 mg/kg
SEX/DURATION :
female 15-21 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,9,1993
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Faceshields;Gloves
Hazard Codes Xn: Harmful;
Risk Phrases R22
RIDADR NONH for all modes of transport
WGK Germany 3.0
RTECS XJ7050340
HS Code 2934999090
HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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