A 77636 hydrochloride |
Catalog No.GC11183 |
Un chlorhydrate de 77636 est un puissant agoniste des récepteurs de la dopamine D1 actif par voie orale, sélectif et à longue durée d'action (pKi \u003d 7,40 ; Ki \u003d 39,8 nM) avec une activité antiparkinsonienne.
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Cas No.: 145307-34-2
Sample solution is provided at 25 µL, 10mM.
A 77636 hydrochloride is a potent and selective agonist of dopamine D1 receptor with Ki value of 39.8 nM [1].
Dopamine D1 receptor is a G-protein couple receptor for dopamine and stimulates adenylate cyclase and cyclic AMP-dependent protein kinases. Dopamine D1 receptor plays an important role in behavioral responses and neuronal growth and development.
A 77636 hydrochloride is a potent and selective dopamine D1 receptor agonist. A-77636 exhibited agonist activities with pEC50 values of 8.13 and 8.97 in the fish retina and the rat caudate-putamen, respectively [1]. In SK-N-MC neuroblastoma cell line, A-77636 significantly induced residual cAMP production [2].
In rats and mice, A-77636 induced forelimb clonus. In marmosets, A-77636 increased locomotor activity and inhibited the parkinsonian-like symptoms induced by MPTP [1]. In rat, A-77636 (4 μmol/kg) significantly increased acetylcholine release in both cortical and hippocampal. However, at a lower dose (1 μmol/kg) A-77636 only stimulated cortical acetylcholine release [3].
References:
[1]. Kebabian JW, Britton DR, DeNinno MP, et al. A-77636: a potent and selective dopamine D1 receptor agonist with antiparkinsonian activity in marmosets. Eur J Pharmacol, 1992, 229(2-3): 203-209.
[2]. Lin CW, Bianchi BR, Miller TR, et al. Persistent activation of the dopamine D1 receptor contributes to prolonged receptor desensitization: studies with A-77636. J Pharmacol Exp Ther, 1996, 276(3): 1022-1029.
[3]. Acquas E, Day JC, Fibiger HC. The potent and selective dopamine D1 receptor agonist A-77636 increases cortical and hippocampal acetylcholine release in the rat. Eur J Pharmacol, 1994, 260(1): 85-87.
Cas No. | 145307-34-2 | SDF | |
Chemical Name | (1R,3S)-3-((1s,3R,5R,7S)-adamantan-1-yl)-1-(aminomethyl)isochroman-5,6-diol hydrochloride | ||
Canonical 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 | ||
Formula | C20H27NO3.HCl | M.Wt | 365.9 |
Solubility | DMF: 33 mg/ml,DMSO: 33 mg/ml,Ethanol: 33 mg/ml,Ethanol:PBS (pH 7.2) (1:6): 0.14 mg/ml | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.733 mL | 13.6649 mL | 27.3299 mL |
5 mM | 0.5466 mL | 2.733 mL | 5.466 mL |
10 mM | 0.2733 mL | 1.3665 mL | 2.733 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5
(Based on Reviews and 27 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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