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| Targets |
SKF-75670 targets the dopamine D1 receptor, a G protein-coupled receptor that is involved in motor control, reward, cognition, and other functions. The compound acts as a selective antagonist at this receptor. By blocking D1 receptor signaling, SKF-75670 can be used to study the role of D1 receptors in various dopamine-dependent processes.
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| ln Vitro |
SKF-75670 is a selective dopamine D1 receptor antagonist. In vitro studies using radioligand binding assays and functional assays have confirmed its affinity and selectivity for D1 receptors over other dopamine receptor subtypes (D2, D3, D4, D5). The compound's antagonist activity has been characterized in various cell-based and tissue-based models.
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| ln Vivo |
When administered intraperitoneally, SKF-75670 hydrochloride (2.5–10 mg/kg) decreases the locomotor activity of marmosets receiving MPTP [2]. Surgical injection of SKF-75670 hydrochloride (0.3 and 1.0 mg/kg) in monkeys with clamp-resistant cocaine: Template change
SKF-75670 has been studied in vivo for its effects on dopamine D1 receptor-mediated behaviors. In animal models, the compound blocks D1 receptor-mediated behaviors such as locomotor activity, stereotypy, and conditioned responses. The compound has been used to investigate the role of D1 receptors in various neurological and psychiatric disorders. |
| Enzyme Assay |
Dopamine D1 receptor binding affinity is assessed using radioligand binding assays with membrane preparations from cells expressing human or rat D1 receptors. Competitive binding experiments are performed using [³H]-SCH-23390 or [³H]-SKF-82957 as radioligands. SKF-75670 is incubated at various concentrations, and Ki values are calculated from displacement curves. Selectivity against D2-like receptors is confirmed using appropriate assays.
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| Cell Assay |
D1 receptor antagonism is assessed in functional assays such as cAMP accumulation assays (D1 receptors are coupled to Gs and stimulate adenylyl cyclase). Cells expressing human D1 receptors are treated with a D1 agonist (e.g., dopamine or SKF-38393) in the presence or absence of SKF-75670. The compound's ability to block agonist-induced cAMP accumulation is measured, and IC50 or Kb values are calculated.
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| Animal Protocol |
Animal/Disease Models: MPTP-treated marmosets [2]
Doses: 2.5-10 mg/kg Route of Administration: peritoneal Intra-injection Experimental Results: diminished locomotor activity (marmosets were essentially immobile and demonstrated sedation and had a flexed posture). SKF-75670 is administered to animals in behavioral studies to assess D1 receptor-mediated effects. Typical routes of administration include intraperitoneal or subcutaneous injection. Behavioral endpoints include locomotor activity, stereotypy, conditioned place preference, and other dopamine-dependent behaviors. The compound is often used in combination with D1 agonists or other dopaminergic agents to elucidate receptor-specific effects. |
| ADME/Pharmacokinetics |
SKF-75670 Hydrobromide has a molecular weight of 350.25 and molecular formula C17H20BrNO2. The IUPAC name is 3-methyl-5-phenyl-1,2,4,5-tetrahydro-3-benzazepine-7,8-diol;hydrobromide. Purity is typically ≥95%. The compound is soluble in DMSO. SKF-75670 is a selective dopamine D1 receptor antagonist and is used as a research tool in neuropharmacology.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of SKF-75670 have not been extensively reported. The compound has been used in animal studies at various doses without significant adverse effects reported. As a D1 receptor antagonist, mechanism-based toxicities may include effects on motor function and cognition. Standard safety precautions should be followed when handling the compound.
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| References |
[1]. Rosenzweig-Lipson S, et al. Dopamine D1 receptor involvement in the discriminative-stimulus effects of SKF 81297 in squirrel monkeys. J Pharmacol Exp Ther. 1993 Nov;267(2):765-75.
[2]. Gnanalingham KK, et al. Differential anti-parkinsonian effects of benzazepine D1 dopamine agonists with varying efficacies in the MPTP-treated common marmoset. Psychopharmacology (Berl). 1995 Feb;117(3):275-86. [3]. Spealman RD, et al. Differential modulation of behavioral effects of cocaine by low- and high-efficacy D1 agonists. Psychopharmacology (Berl). 1997 Oct;133(3):283-92. |
| Additional Infomation |
SKF-75670 Hydrobromide (CAS#: 62717-63-9) is a selective dopamine D1 receptor antagonist. It is primarily used as a research tool in neuropharmacology to study dopamine-related pathways in the brain. The compound has been studied for its potential effects on dopamine D1 receptor-mediated behaviors and physiological processes. SKF-75670 is a member of the benzazepine class of dopamine receptor ligands and is intended for research use only.
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| Molecular Formula |
C17H19NO2.HBR
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| Molecular Weight |
350.2502
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| Exact Mass |
349.068
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| CAS # |
62717-63-9
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| Related CAS # |
62717-63-9 (HBr);104114-24-1;
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| PubChem CID |
173870
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| Appearance |
White to yellow solid powder
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| Boiling Point |
450.1ºC at 760 mmHg
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| Flash Point |
241ºC
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| LogP |
3.613
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
316
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCc2cc(c(cc2C(C1)c3ccccc3)O)O.Br
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| InChi Key |
KWTPHNVUAVFKGB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H19NO2.BrH/c1-18-8-7-13-9-16(19)17(20)10-14(13)15(11-18)12-5-3-2-4-6-12;/h2-6,9-10,15,19-20H,7-8,11H2,1H3;1H
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| Chemical Name |
3-methyl-5-phenyl-1,2,4,5-tetrahydro-3-benzazepine-7,8-diol;hydrobromide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~40 mg/mL (~114.20 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.14 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.14 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8551 mL | 14.2755 mL | 28.5510 mL | |
| 5 mM | 0.5710 mL | 2.8551 mL | 5.7102 mL | |
| 10 mM | 0.2855 mL | 1.4276 mL | 2.8551 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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