Alverine Citrate (Synonyms: NSC 35459) |
رقم الكتالوجGC10891 |
Alverine citrate هو مضاد لمستقبلات 5-HT1A ، مع IC50 من 101 نانومتر
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Cas No.: 5560-59-8
Sample solution is provided at 25 µL, 10mM.
Alverine citrate is a 5-HT1A receptor antagonist, with an IC50 of 101 nM.
Alverine is a drug used for functional gastrointestinal disorders. Alverine acts directly on the muscle in the gut, causing it to relax. Alverine Citrate (20 mg/kg) suppresses the effect of 5-HTP, but not that of 8-OH-DPAT. However, when injected intracerebroventricularly (75 μg/rat) alverine citrate reduces 8-OH-DPAT-induced enhancement of rectal distension-induced abdominal contractions. In-vitro binding studies reveal that Alverine citrate has a high affinity for 5-HT1A receptors and a weak affinity for 5-HT3 and 5-HT4 subtypes[1]. Alverine may increase Ca influx during action potentials due to inhibition of the inactivation of L-type Ca channels, but may also suppress evoked activity by inhibiting the sensitivity of contractile proteins to Ca2+[2].
References:
[1]. Coelho, A.M., et al., Rectal antinociceptive properties of alverine citrate are linked to antagonism at the 5-HT1A receptor subtype. J Pharm Pharmacol, 2001. 53(10): p. 1419-26.
[2]. Hayase, M., et al., Evolving mechanisms of action of alverine citrate on phasic smooth muscles. Br J Pharmacol, 2007. 152(8): p. 1228-38.
Cas No. | 5560-59-8 | SDF | |
المرادفات | NSC 35459 | ||
Chemical Name | N-ethyl-3-phenyl-N-(3-phenylpropyl)propan-1-amine;2-hydroxypropane-1,2,3-tricarboxylic acid | ||
Canonical SMILES | CCN(CCCC1=CC=CC=C1)CCCC2=CC=CC=C2.C(C(=O)O)C(CC(=O)O)(C(=O)O)O | ||
Formula | C20H27N.C6H8O7 | M.Wt | 473.56 |
الذوبان | ≥ 23.68mg/mL in DMSO | 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 | 2.1117 mL | 10.5583 mL | 21.1166 mL |
5 mM | 0.4223 mL | 2.1117 mL | 4.2233 mL |
10 mM | 0.2112 mL | 1.0558 mL | 2.1117 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: >99.00%
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Average Rating: 5
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