Alniditan
Alniditan (Alnitidan) is a potent 5-HT1B and 5-HT1D receptors agonist, with IC50s of 1.7 nM and 1.3 nM for h5-HT1B and h5-HT1D receptors in HEK293 cells, respectively. Alniditan has migraine-preventive effects.
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- CAS. Nr.: 152317-89-0
- Formel: C17H26N4O
- Molecular Weight:302.41
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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human 5-HT1B Receptor 1.7 nM (IC50, in HEK 293 cell) |
human 5-HT1D Receptor 1.3 nM (IC50, in HEK 293 cell) |
5-HT1B Receptor 0.9 nM (Kd) |
5-HT1D Receptor 1.2 nM (Kd) |
In vitro, Alniditan exhibits little vasoconstrictive effects on the rat basilar artery, although at a very high concentration 1 mM, Alniditan causes intensive constriction, most likely through a mechanism independent from 5-HT receptor activation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 152317-89-0
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Molecular Weight 302.41
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Formel C17H26N4O
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SMILES
C1(NCCCNC[C@H]2CCC3=CC=CC=C3O2)=NCCCN1
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Synonyms
Alnitidan
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
After a stabilisation period of about 1 h, the animals are divided into three groups. In the first group (n=4), values of heart rate, mean arterial blood pressure, carotid blood flow and its distribution, as well as arterial and jugular venous blood gases are measured at baseline, and after four consecutive injections of physiological saline (0.5 mL, every 20 min). The second and third groups of animals (n=6 each) are pre-treated with saline (i.v.) or GR127935 (0.5 mg/kg, i.v.), respectively, given over a period of 5 min at a rate of 1 mL/min. After a waiting period of 15 min, baseline values of heart rate, mean arterial blood pressure, carotid blood flow and its distribution, as well as arterial and jugular venous blood gases are measured. Subsequently, these groups of animals receive sequential i.v. doses of alniditan (3, 10, 30 and 100 μg/kg) every 20 min. Fifteen minutes after each dose of alniditan, all haemodynamic variables are assessed again.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
Verweise
[1]. Limmroth V, et al. Effects of alniditan on neurogenic oedema in the rat dura mater and on contraction of rat basilar artery. Eur J Pharmacol. 1999 Oct 8;382(2):103-9. [Content Brief]
[2]. Lesage AS, et al. Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Br J Pharmacol. 1998 Apr;123(8):1655-65. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)