GLPBio

A 77636 hydrochloride

Catalog No.: GC11183Purity:>99.50%
COASDSData Sheet
Un clorhidrato de 77636 es un potente agonista del receptor de dopamina D1, activo por vía oral, selectivo y de acción prolongada (pKi \u003d 7,40; Ki \u003d 39,8 nM) con actividad antiparkinsoniana.

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A 77636 hydrochloride
Cas No.: 145307-34-2
1mgIn Stock
$69.00
1
5mgIn Stock
$248.00
1
10mgIn Stock
$362.00
1
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Descripción (Description)

A 77636 hydrochloride is a selective dopamine D1 receptor agonist with pKi=7.40±0.09; Ki=39.8nM and EC50=1.1nM. A 77636 is commonly used in Parkinson's disease research [1].

In vitro, pretreatment of SK-N-MC cells with A 77636 (200nM; 1h) led to a persistent elevation of cAMP levels, and can be blocked by SCH 23390 [2]. A 77636 (1-20μM) upregulated the phosphorylation of eIF2α, inhibited proliferation, motility, and bone metastatic activity of 4T1.2 mammary tumor cells and MDA-MB-231 breast cancer cells [3].

In vivo, A 77636 (3μmole/kg; s.c.) increased locomotor activity and decreased the severity of the parkinsonian-like symptoms in marmosets treated with MPTP (1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine) induced parkinsonian-like model [1]. A 77636 (3-60mg/kg; s.c.) increased horizontal locomotion and rearing at lower doses in Male hD1 mice [4]. A 77636 (3 and 10mg/kg; i.p.) produced dose-related attenuation and decreased peak responding to cocaine in Swiss-Webster mice [5]. A 77636 (0.1–1.0mg/kg, s.c.) exerted a suppressant effect on food intake in rat, due to a reduction in meal size and duration [6].

References:
[1]. Kebabian, John W., et al. "A 77636: a potent and selective dopamine D1 receptor agonist with antiparkinsonian activity in marmosets." European journal of pharmacology 229.2-3 (1992): 203-209.
[2]. Lin, Chun Wel, et al. "Persistent activation of the dopamine D1 receptor contributes to prolonged receptor desensitization: studies with A 77636." The Journal of pharmacology and experimental therapeutics 276.3 (1996): 1022-1029.
[3]. Minami, Kazumasa, et al. "Inhibitory effects of dopamine receptor D1 agonist on mammary tumor and bone metastasis." Scientific reports 7.1 (2017): 45686.
[4]. Svensson, Kjell A., et al. "An allosteric potentiator of the dopamine D1 receptor increases locomotor activity in human D1 knock-in mice without causing stereotypy or tachyphylaxis." The Journal of pharmacology and experimental therapeutics 360.1 (2017): 117-128.
[5]. Chausmer, Allison L., and Jonathan L. Katz. "Comparison of interactions of D1-like agonists, SKF 81297, SKF 82958 and A 77636, with cocaine: locomotor activity and drug discrimination studies in rodents." Psychopharmacology 159.2 (2002): 145-153.

Protocolo (Protocol)

Cell experiment [1]:

Cell lines

MDA-MB-231 cells

Preparation Method

4T1.2 mouse mammary tumor cells were cultured in DMEM, the culture media contained 10% fetal bovine serum (FBS) and antibiotics (50units/ml penicillin, and 50μg/ml streptomycin). Cells were maintained at 37°C and 5% CO2 in a humidified incubator. Then add 2, 5, and 10μM A 77636 in the culture media for 32-48h.

Reaction Conditions

2, 5, and 10μM; 32-48h

Applications

A 77636 (2, 5, and 10 μM) reduced the cellular motility of MDA-MB-231 cells in a dose-dependent manner in the wound healing scratch assay.
Animal experiment [2]:

Animal models

Male hD1 mice, 8–10 weeks old

Preparation Method

Mice were placed inside individual locomotor activity (LMA) boxes for 1 hour during an acclimation period. Mice were then dosed with test compounds (oral or subcutaneous) and were replaced inside individual LMA boxes for the start of LMA. Photocell activity (total ambulations) was collected for 60 minutes using software from Hamilton Kinder. DETQ was dissolved in 20% 2-hydroxypropyl-β-cyclodextrin, and D1 agonists SKF 82958 and A 77636 and D1 antagonist SCH39166 were dissolved in 0.9% dihydrexidine saline.

Dosage form

3-60mg/kg; s.c.

Applications

The D1 agonists SKF 82958 and A 77636 showed an increase in horizontal locomotion and rearing at lower doses.

References:
[1]. Minami, Kazumasa, et al. "Inhibitory effects of dopamine receptor D1 agonist on mammary tumor and bone metastasis." Scientific reports 7.1 (2017): 45686.
[2]. Svensson, Kjell A., et al. "An allosteric potentiator of the dopamine D1 receptor increases locomotor activity in human D1 knock-in mice without causing stereotypy or tachyphylaxis." The Journal of pharmacology and experimental therapeutics 360.1 (2017): 117-128.

Documentos del producto (Product Documents)

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Propiedades químicas (Chemical Properties)

N.º CAS
145307-34-2
Nombre químico
(1R,3S)-3-((1s,3R,5R,7S)-adamantan-1-yl)-1-(aminomethyl)isochroman-5,6-diol hydrochloride
SMILES
OC(C1=C(C=C2)[C@H](CN)O[C@@H](C1)[C@]3(C[C@H](C4)C5)C[C@@H]4C[C@H]5C3)=C2O.Cl
Fórmula molecular
C20H27NO3.HCl
Peso molecular
365.9
Solubilidad
DMF: 33 mg/ml,DMSO: 33 mg/ml,Ethanol: 33 mg/ml,Ethanol:PBS (pH 7.2) (1:6): 0.14 mg/ml
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

Reviews

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