Dayang Chem (Hangzhou) Co., Ltd.
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Product Name: Talipexole dihydrochloride
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Purity: 98.0%
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36085-73-1

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: 2026-07-12 22:55:57
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	5,6,7,8-Tetrahydro-6-(2-propenyl)-4H-thiazolo[4,5-d]azin-2-amine Dihydrochloride, 6-Allyl-2-amino-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azine Dihydrochloride Talipexoledihydrochloride B-HT 920 DIHYDROCHLORIDE A2 ADRENOCTOR AGONI 5,6,7,8-Tetrahydro-6-(2-propen-1-yl)-4H-thiazolo[4,5-d] azin-2-amine dihydrochloride 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azine-2-amine dihydrochloride Talipexole dihydrochloride, 10 mM in DMSO 5,6,7,8-TETRAHYDRO-6-(2-PROPENYL)-4H-THIAZOLO[4,5-D]AZINE-2-AMINE DIHYDROCHLORIDE Talipexole 2HCl 4H-Thiazolo[4,5-d]azepin-2-amine, 5,6,7,8-tetrahydro-6-(2-propen-1-yl)-, hydrochloride (1:2) talipexole hydrochloride Talipexole, 5,6,7,8-Tetrahydro-6-(2-propenyl)-4H-thiazolo[4,5-d]azine-2-amine dihydrochloride 5,6,7,8-Tetrahydro-6-(2-propenyl)-4H-thiazolo[4,5-d]azin-2-amineDihydrochloride,6-Allyl-2-amino-5,6,7,8-tetrahydro-4 talipexoledihydrochloride hydrochloride (1:2) 6-ALLYL-2-AMINO-5,6,7,8-TETRAHYDRO-4H-THIAZOLO[4,5-D]AZINE DIHYDROCHLORIDE b-ht920 5-d)azin-2-amine,5,6,7,8-tetrahydro-6-(2-propenyl)-4h-thiazolo(dihydroch Hydrochloric talipexole B-HT920dihydrochlorideTalipexole 5,6,7,8-tetrahydro-6-(2-propenyl)-4h-thiazolo(4,5-d)azin-2-aminedihydrochl B-HT 920 dihydrochloride 5,6,7,8-TETRAHYDRO-6-(2-PROPENYL)-4H-THIAZOLO[4,5-D]AZIN-2-AMINE DIHYDROCHLORIDE 4H-Thiazolo(4,5-D)azin-2-amine, 5,6,7,8-tetrahydro-6-(2-propenyl)-, dihydrochloride 6-Allyl-5,6,7,8-tetrahydro-4H-[1,3]thiazolo[4,5-d]azepin-2-amine dihydrochloride 2-amino-6-allyl-4,5,7,8-tetrahydro-6h-thiazolo(5,4-d)azin-dihydrochlorid B-HT 920 2HCl B-HT 920 DIHYDROCHLORIDE B-HT 920 Dihydrochloride\nTalipexole B-HT 920 (hydrochloride) 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azin-2-amine dihydrochloride MFCD00274573 4H-Thiazolo[4,5-d]azin-2-amine, 5,6,7,8-tetrahydro-6-(2-propen-1-yl)-, hydrochloride (1:2) Talipexole dihydrochloride 4H-Thiazolo[4 Domin Talipexole Talipexole HCl 5,6,7,8-Tetrahydro-6-(2-propenyl)-4H-thiazolo[4,5-d]azepine-2-amine dihydrochloride 8-tetrahydro-6-(2-propen-1-yl) 6-Allyl-5,6,7,8-tetrahydro-4H-thiazole [4,5-d] aza-2-amine dihydrochloride 5-d]azin-2-aMine 2-Amino-6-allyl-4,5,7,8-tetrahydro-6H-thiazolo(5,4-D)azin-dihydrochlorid [german] TALIPEXOLE DIDHYDROCHLORIDE

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	Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Neurological Disease
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
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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