2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Almotriptan

Almotriptan  (Synonyms: PNU180638 free base)

Cat. No.: HY-B0383A Purity: 99.18%
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Almotriptan (PNU180638 free base) is an orally active, highly selective agonist of the 5-HT1B/1D receptor (5-HT1B/1D receptor), with EC50 values of 1.6 nM and 3.1 nM, respectively. Almotriptan shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan can be used in research related to migraine.

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Almotriptan

Almotriptan Chemical Structure

CAS No. : 154323-57-6

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Almotriptan Related Antibodies

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Description

Almotriptan (PNU180638 free base) is an orally active, highly selective agonist of the 5-HT1B/1D receptor (5-HT1B/1D receptor), with EC50 values of 1.6 nM and 3.1 nM, respectively. Almotriptan shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan can be used in research related to migraine[1][2].

IC50 & Target

5-HT1B Receptor

 

5-HT1D Receptor

 

In Vitro

Almotriptan acts as a full agonist to induce potent concentration-dependent contractions in canine isolated saphenous veins, with an EC50 of 394 nM, via 5-HT1B/1D receptors[2].
Almotriptan induces vasoconstriction in human isolated meningeal, superficial temporal, and basilar arteries, with EC50 values of 0.7 μM (superficial temporal) and 3.7 μM (basilar), and greater potency than Sumatriptan (HY-B0121B) in meningeal arteries[2].
Almotriptan is metabolized by multiple human liver microsomal enzymes, including MAO-A, FMO, aldehyde dehydrogenase, CYP2D6, and CYP3A4, and only weakly inhibits CYP2D6 with no significant inhibition of MAO-A or MAO-B[2].

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

Almotriptan Related Antibodies
In Vivo

Almotriptan (0.01-3000 μg/kg; intravenous/intradermal administration; single dose) increases carotid vascular resistance in anesthetized cats, with efficacy and potency comparable to those of Sumatriptan; it elevates resistance by 100% at an intravenous dose of 9 μg/kg and exerts effects via the 5-HT1 receptor[2].
Almotriptan (0-1 mg/kg; intravenous injection; single dose; maximum 0.3 mg/kg; intravenous injection; single dose; 30 μg/min; intracoronary infusion; 1 h) increases carotid vascular resistance in beagle dogs, and exhibits better carotid-femoral artery selectivity than Sumatriptan. At the tested doses, this agent has favorable cardiovascular safety, with no cardiac inhibitory effect or QTc interval change[2].
Almotriptan (10 mg/kg; subcutaneous injection; single dose) inhibits trigeminal ganglion-induced meningeal vascular extravasation in anesthetized guinea pigs, and at a subcutaneous dose of 10 mg/kg, it causes no hypothermia or bronchospasm in conscious guinea pigs[2].
Almotriptan (oral administration; single dose) does not alter cardiovascular parameters or diuretic effects in normotensive Wistar rats at the tested oral doses[2].
Almotriptan (1-3 mg/kg; subcutaneous injection; single administration) exerts no cardiovascular effects at the dose of 1 mg/kg s.c. in conscious cynomolgus monkeys, while the 3 mg/kg s.c. dose only induces mild, transient effects without electrocardiogram changes[2].
Almotriptan (up to 300 mg/kg; p.o.; single administration) shows no central nervous system-related behavioral or motor function effects in mice at oral doses up to 300 mg/kg[2].
Almotriptan slightly alleviates apomorphine (HY-12723)-induced vomiting responses in dogs[2].

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

335.46

Formula

C17H25N3O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(CC1=CC2=C(NC=C2CCN(C)C)C=C1)(N3CCCC3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (298.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9810 mL 14.9049 mL 29.8098 mL
5 mM 0.5962 mL 2.9810 mL 5.9620 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.18%

SDS (394 KB)

COA (249 KB) HNMR (266 KB) LCMS (333 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9810 mL 14.9049 mL 29.8098 mL 74.5245 mL
5 mM 0.5962 mL 2.9810 mL 5.9620 mL 14.9049 mL
10 mM 0.2981 mL 1.4905 mL 2.9810 mL 7.4525 mL
15 mM 0.1987 mL 0.9937 mL 1.9873 mL 4.9683 mL
20 mM 0.1490 mL 0.7452 mL 1.4905 mL 3.7262 mL
25 mM 0.1192 mL 0.5962 mL 1.1924 mL 2.9810 mL
30 mM 0.0994 mL 0.4968 mL 0.9937 mL 2.4842 mL
40 mM 0.0745 mL 0.3726 mL 0.7452 mL 1.8631 mL
50 mM 0.0596 mL 0.2981 mL 0.5962 mL 1.4905 mL
60 mM 0.0497 mL 0.2484 mL 0.4968 mL 1.2421 mL
80 mM 0.0373 mL 0.1863 mL 0.3726 mL 0.9316 mL
100 mM 0.0298 mL 0.1490 mL 0.2981 mL 0.7452 mL
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Almotriptan Related Classifications

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.

Keywords:

Almotriptan154323-57-6PNU180638PNU 180638PNU-1806385-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT1B receptorsmigrainecytochrome P450 2D65-HT1F receptorstrigeminal nerve endings5-HT1D receptorstrigeminocervical complex5-HT1B/1D receptor5-HT1A receptorscytochrome P450 3A4Inhibitorinhibitorinhibit

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