1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. 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 HEK 293 cells, respectively. Alniditan has migraine-preventive effects.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Alniditan dihydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

Alniditan Chemical Structure

Alniditan Chemical Structure

CAS No. : 152317-89-0

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Description

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 HEK 293 cells, respectively. Alniditan has migraine-preventive effects[1][2].

IC50 & Target[2]

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

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.

In Vivo

The intraperitoneal administration of Alniditan ED50=9 μg/kg dose dependly reduces [125I]-BSA extravasation in the rat meninges when done 30 min before stimulation. Alniditan dose dependently attenuateds the neurogenic inflammation in vivo model of neurogenic inflammation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

302.41

Formula

C17H26N4O

CAS No.
SMILES

C1(NCCCNC[C@H]2CCC3=CC=CC=C3O2)=NCCCN1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
Animal Administration
[2]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Alniditan Related Classifications

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This equation is commonly abbreviated as: C1V1 = C2V2

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Alniditan
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HY-101698
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