| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
GR 55562 targets 5-HT₁B and 5-HT₁D serotonin receptors as a selective antagonist. It binds with high affinity to these receptors, blocking the effects of endogenous serotonin. By antagonizing 5-HT₁B/₁D receptors, GR 55562 modulates serotonergic neurotransmission and has been used to study the role of these receptors in various central nervous system functions including regulation of mood, anxiety, pain perception, and vasoconstriction. The compound is often used to differentiate 5-HT₁B/₁D receptor-mediated effects from those mediated by other serotonin receptor subtypes.
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| ln Vitro |
In vitro, GR 55562 demonstrates high affinity binding to 5-HT₁B and 5-HT₁D receptors in radioligand binding assays. It effectively blocks serotonin-induced activation of these receptors, inhibiting downstream signaling pathways such as inhibition of adenylate cyclase. The compound has been used in functional assays to characterize the pharmacological profile of 5-HT₁B/₁D receptors and to differentiate their roles from other serotonin receptor subtypes. Selectivity studies have confirmed its specificity for 5-HT₁B/₁D receptors.
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| ln Vivo |
In the accumbens region, GR 55562 (0.1–10 μg/side) does not cause a cocaine lever response [1]. The enlightening effects of cocaine are considerably disrupted when GR 55562 (0.1-10 μg/side) (in the nucleus accumbens shell or core) fails to modify it [1].
In vivo, GR 55562 has been used in animal models to investigate the role of 5-HT₁B/₁D receptors in migraine, depression, and anxiety. It modulates serotonergic neurotransmission in various brain regions. The compound has been instrumental in understanding the mechanisms of action of triptan drugs used for migraine treatment, which act as 5-HT₁B/₁D receptor agonists. GR 55562 has also been studied for its effects on cardiovascular function and pain perception. |
| Enzyme Assay |
Radioligand binding assays: Membranes from cells expressing 5-HT₁B or 5-HT₁D receptors are incubated with a radiolabeled ligand (e.g., [³H]-GR 125743 or [³H]-5-HT) and GR 55562 at various concentrations (typically 0.1-100 nM). Binding affinity (Kᵢ) is calculated from displacement curves. Selectivity is assessed by testing against other serotonin receptor subtypes and unrelated receptors.
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| Cell Assay |
Cells expressing recombinant 5-HT₁B/₁D receptors (e.g., CHO or HEK293 cells) are cultured in appropriate media. For functional assays, cells are pre-incubated with GR 55562 and then stimulated with serotonin. Receptor activation is assessed by measuring inhibition of forskolin-stimulated cAMP accumulation using ELISA or HTRF-based detection kits. IC₅₀ values are calculated from dose-response curves.
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| Animal Protocol |
Animal/Disease Models: Male Wistar rats (280-300 g; n=50)[1] ].
Doses: 0.1-10 μg/side. Route of Administration: intracranial injection; volume 0.2 µl/side. Experimental Results: No intravesicular shell infusion drug induced Substitution. Did not Dramatically affect the discriminative stimulus effects produced by 5 mg/kg cocaine. GR 55562 (1 µg/side) attenuated the cumulative intra-core CP 93129 (1 µg/side) and systemic cocaine (1.25 mg/kg or 2.5 mg/kg ) combination-induced enhancement of cocaine discrimination. In vivo studies are conducted in rodent models. GR 55562 is administered via intraperitoneal, subcutaneous, or intracerebroventricular injection at specified doses. Behavioral tests (e.g., elevated plus maze for anxiety, forced swim test for depression, and migraine models) are performed. Microdialysis is used to measure neurotransmitter levels in brain regions. Cardiovascular parameters are monitored in relevant models. |
| ADME/Pharmacokinetics |
GR 55562 dihydrochloride is a selective 5-HT₁B/₁D receptor antagonist with high affinity (pKᵢ values typically in the low nanomolar range). It is soluble in DMSO and water. The compound is stable under recommended storage conditions and is suitable for both in vitro and in vivo pharmacological research. Detailed physicochemical properties are available from chemical suppliers.
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| References | |
| Additional Infomation |
GR 55562 dihydrochloride is a selective antagonist of 5-HT₁B and 5-HT₁D serotonin receptors. It has been used in pharmacological research to study the role of these receptors in various physiological and pathological processes including migraine, depression, anxiety, and cardiovascular function. The compound has been instrumental in understanding the mechanisms of action of triptan drugs and in characterizing the pharmacological profile of 5-HT₁B/₁D receptors.
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| Molecular Formula |
C23H27CL2N3O2
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|---|---|
| Molecular Weight |
448.385383844376
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| Exact Mass |
447.148
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| CAS # |
159533-25-2
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| Related CAS # |
GR 55562 hydrochloride;172854-55-6
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| PubChem CID |
56972159
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
471
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)CCCC1=C(C=CC(=C1)C(=O)NC2=CC=C(C=C2)C3=CC=NC=C3)O.Cl.Cl
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| InChi Key |
KBKWJHYQFQONBJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H25N3O2.2ClH/c1-26(2)15-3-4-19-16-20(7-10-22(19)27)23(28)25-21-8-5-17(6-9-21)18-11-13-24-14-12-18;;/h5-14,16,27H,3-4,15H2,1-2H3,(H,25,28);2*1H
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| Chemical Name |
3-[3-(dimethylamino)propyl]-4-hydroxy-N-(4-pyridin-4-ylphenyl)benzamide;dihydrochloride
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2302 mL | 11.1510 mL | 22.3020 mL | |
| 5 mM | 0.4460 mL | 2.2302 mL | 4.4604 mL | |
| 10 mM | 0.2230 mL | 1.1151 mL | 2.2302 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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