A 77636 hydrochlorideAgonist of D1-like dopamine receptor,potent and selective CAS# 145307-34-2 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 145307-34-2 | SDF | Download SDF |
| PubChem ID | 64637 | Appearance | Powder |
| Formula | C20H28ClNO3 | M.Wt | 365.9 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in water | ||
| Chemical Name | (1R)-3-(1-adamantyl)-1-(aminomethyl)-3,4-dihydro-1H-isochromene-5,6-diol;hydrochloride | ||
| SMILES | C1C2CC3CC1CC(C2)(C3)C4CC5=C(C=CC(=C5O)O)C(O4)CN.Cl | ||
| Standard InChIKey | BWHPNJVKFAPVOG-LXJUREGMSA-N | ||
| Standard InChI | InChI=1S/C20H27NO3.ClH/c21-10-17-14-1-2-16(22)19(23)15(14)6-18(24-17)20-7-11-3-12(8-20)5-13(4-11)9-20;/h1-2,11-13,17-18,22-23H,3-10,21H2;1H/t11?,12?,13?,17-,18?,20?;/m0./s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent and selective dopamine D1-like receptor agonist (pEC50 values are 8.97 and < 5 for D1-like and D2-like receptors respectively). Displays anti-Parkinsonian activity following oral administration in vivo. |
A 77636 hydrochloride Dilution Calculator
A 77636 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.733 mL | 13.6649 mL | 27.3299 mL | 54.6597 mL | 68.3247 mL |
| 5 mM | 0.5466 mL | 2.733 mL | 5.466 mL | 10.9319 mL | 13.6649 mL |
| 10 mM | 0.2733 mL | 1.3665 mL | 2.733 mL | 5.466 mL | 6.8325 mL |
| 50 mM | 0.0547 mL | 0.2733 mL | 0.5466 mL | 1.0932 mL | 1.3665 mL |
| 100 mM | 0.0273 mL | 0.1366 mL | 0.2733 mL | 0.5466 mL | 0.6832 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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Homologous desensitization of the D1A dopamine receptor: efficacy in causing desensitization dissociates from both receptor occupancy and functional potency.[Pubmed:9655879]
J Pharmacol Exp Ther. 1998 Jul;286(1):345-53.
The role of drug efficacy in agonist-induced desensitization was studied in C-6 glioma cells transfected with the monkey dopamine D1A (mD1A) receptor. Dopamine pretreatment for 2 hr produced greater than 80% loss of responsiveness in the stimulation of cAMP accumulation that was blocked by the D1 antagonist SCH23390. A series of full and partial D1 agonists from structurally dissimilar classes were then examined. Three full agonists (dihydrexidine, SKF82958, A77636) desensitized the receptor to the same extent as dopamine, whereas two other full agonists (dinapsoline and A68930) and all the partial agonists tested (SKF38393, pergolide and d-lysergic acid diethylamide tartrate) produced only partial desensitization (i.e., 50% that of dopamine). Whereas partial agonists (i.e., SKF38393, pergolide and d-lysergic acid diethylamide tartrate) caused no alteration in ligand-accessible mD1A receptors, four of the full agonists (dopamine, dihydrexidine, dinapsoline, A68930) caused a 30 to 40% reduction in receptor number. One full agonist, A77636, caused nearly an 80% decrease in receptor number, despite the fact that the degree of functional desensitization was similar to the other full agonists. The desensitization of the D1 receptor was homologous, not affecting beta-2 adrenergic receptors endogenous to C-6 cells. Neither incubation with cAMP analogs, nor inhibition of protein kinase A, affected dopamine-induced desensitization, suggesting a cAMP-independent mechanism in this cell line. Together, these data suggest that functional desensitization of the mD1A receptor expressed in C-6 glioma cells is a cAMP-independent mechanism, cannot be predicted reliably from agonist efficacy for stimulating adenylate cyclase and can occur in the absence of changes in receptor number.
The potent and selective dopamine D1 receptor agonist A-77636 increases cortical and hippocampal acetylcholine release in the rat.[Pubmed:7957630]
Eur J Pharmacol. 1994 Jul 21;260(1):85-7.
The effects of systemic administration of the full dopamine D1 receptor agonist A-77636 on acetylcholine release in rat frontal cortex and hippocampus were studied using in vivo microdialysis. Administration of A-77636 (4 mumol/kg s.c.) greatly (> 230%) increased both cortical and hippocampal acetylcholine release for more than 3 h; at a lower dose (1 mumol/kg s.c.) A-77636 significantly stimulated cortical but not hippocampal acetylcholine release. The effect of the higher dose of A-77636 on cortical acetylcholine release was blocked by the dopamine D1 receptor antagonist SCH 23390 (300 micrograms/kg s.c.). These results confirm that stimulation of dopamine D1 receptors facilitates cortical and hippocampal acetylcholine release in vivo, and indicate that these two structures are differentially sensitive to this effect. They also raise the possibility that dopamine D1 receptor agonists may be useful in the treatment of cortical and hippocampal acetylcholine deficit-related syndromes.
A-77636: a potent and selective dopamine D1 receptor agonist with antiparkinsonian activity in marmosets.[Pubmed:1362704]
Eur J Pharmacol. 1992 Dec 15;229(2-3):203-9.
A-77636, ((1R,3S) 3-(1'-adamantyl)-1-aminomethyl-3,4-dihydro-5,6-dihydroxy-1H-2-benz opyran hydrochloride), is a selective dopamine D1 receptor agonist. In a battery of receptor binding assays, A-77636 shows the highest affinity (pKi = 7.40 +/- 0.09; Ki = 39.8 nM) for the dopamine D1 receptor. A-77636 is an agonist at the dopamine D1 receptors in the fish retina (pEC50 = 8.13; EC50 = 1.1 nM; intrinsic activity = 102% of dopamine) and the rat caudate-putamen (pEC50 = 8.97; intrinsic activity = 134% of dopamine). The compound is functionally inactive at dopamine D2 receptors (EC50 > 10 microM). In rats with unilateral 6-OHDA (6-hydroxydopamine) lesions of the nigro-striatal dopaminergic pathway, A-77636 elicits prolonged (> 20 h) contralateral turning that is blocked by SCH 23390, a D1 receptor antagonist, but not by haloperidol at doses selective for the dopamine D2 receptor. Higher doses of A-77636 produce forelimb clonus in rats and mice. When tested in marmosets treated with MPTP to induce a parkinsonian-like state, A-77636 increases locomotor activity and decreases the severity of the parkinsonian-like symptoms: the compound is active after either subcutaneous or oral administration. A-77641, the optical antipode of A-77636, has a lower affinity towards the dopamine D1 receptor (pKi = 5.14, Ki = 7200 nM), is less potent as a dopamine D1 receptor agonist (pEC50 = 5.65; EC50 = 2200 nM), fails to elicit turning in the 6-OHDA-lesioned rat, and lacks antiparkinsonian efficacy in the MPTP-treated marmoset.(ABSTRACT TRUNCATED AT 250 WORDS)
