Tiamenidine
Tiamenidine (HOE 440) is an orally active α-2 adrenoceptor agonist. Tiamenidine stimulates peripheral α-adrenergic receptors, causing a transient increase in blood pressure, and activates central adrenergic receptors, inhibiting sympathetic nerve activity. Tiamenidine lowers blood pressure in hypertensive rats and inhibits plasma renin activity. Tiamenidine reduces ethanol preference and intake in ethanol-preferring rats. Tiamenidine attenuates Xylazine-induced loss of righting reflex. Tiamenidine can be used in research on hypertension.
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- CAS No.: 31428-61-2
- Formule: C8H10ClN3S
- Masse moléculaire:215.70
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Activité biologique
Description
IC50 & Target
IC50: α2-Adrenergic Receptor[1]
In Vivo
Tiamenidine reduces blood pressure, plasma norepinephrine, epinephrine, and plasma renin activity[2].
Tiamenidine (0.04-10 mg/kg; subcutaneous injection; single administration) partially antagonizes Xylazine-induced loss of righting reflex, but does not produce complete blockade[3].
Tiamenidine produces partial central nervous system depression, moderate muscle relaxation, and hypothermia in healthy rats, with an ED50 value of 0.73 mg/kg for impairment of the righting reflex, 0.12 mg/kg for muscle relaxation, and 0.32 mg/kg for hypothermia[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (female, 220-270 g)[3]
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Dosage:0.04, 0.16, 0.63, 2.5, and 10 mg/kg
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Administration:s.c.; single administration; 60 min before observation
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Result:Partially antagonized xylazine‑induced loss of righting reflex with ED50 = 1.7 mg/kg.
Chemical Information
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CAS No. 31428-61-2
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Masse moléculaire 215.70
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Formule C8H10ClN3S
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SMILES
CC1=CSC(Cl)=C1NC2=NCCN2
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Synonyms
HOE 440
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tiamenidine Related Classifications
HY-112074 Related Classifications
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