Almotriptan hydrochloride 

Almotriptan (PNU180638) hydrochloride is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan hydrochloride shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan hydrochloride induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan hydrochloride can be used in research related to migraine.

Almotriptan hydrochloride 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 hydrochloride 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 hydrochloride 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 (0.01-3000 μg/kg; intravenous/intradermal administration; single dose) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride shows no central nervous system-related behavioral or motor function effects in mice at oral doses up to 300 mg/kg^[2].
Almotriptan hydrochloride 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.

371.93

C₁₇H₂₆ClN₃O₂S

154323-46-3

CN(CCC1=CNC2=C1C=C(CS(=O)(N3CCCC3)=O)C=C2)C.Cl

Room temperature in continental US; may vary elsewhere.

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

• [1]. Pascual J, et al. Almotriptan: a review of 20 years' clinical experience. Expert Rev Neurother. 2019;19(8):759-768.  [Content Brief]

  [2]. Gras J, et al. Almotriptan, a new anti-migraine agent: a review. CNS Drug Rev. 2002;8(3):217-234.  [Content Brief]