1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. Cevimeline

Cevimeline (Synonyms: AF102B)

Cat. No.: HY-70020
Handling Instructions

Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline can cross the blood-brain barrier (BBB).

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

Cevimeline Chemical Structure

Cevimeline Chemical Structure

CAS No. : 107233-08-9

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Description

Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia[1][2][3][4]. Cevimeline can cross the blood-brain barrier (BBB)[5].

IC50 & Target

Muscarinic M1 and M3 receptor[1]

In Vitro

In digested parotid cells, Cevimeline (0.1-100 μM) increases the intracellular Ca2+ concentration[1].

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

In Vivo

Cevimeline (0.008-0.016 mg/kg; intraperitoneal injection; male Wistar rats) treatment shows slowly increasing and lasting salivation, and increased blood flow increment in the parotid gland and pressor response. Cevimeline inhibits angiotensin II-induced water intake and neuronal activity in the subfornical organ at 0.016 mg/kg[1].

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

Animal Model: Male Wistar rats (8-week-old) injected with angiotensin-II[1]
Dosage: 0.008 mg/kg, 0.016 mg/kg
Administration: Intraperitoneal injection
Result: Showed slowly increasing and lasting salivation, and increased blood flow increment in the parotid gland and pressor response.
Clinical Trial
Molecular Weight

199.31

Formula

C₁₀H₁₇NOS

CAS No.
SMILES

C[[email protected]]1SC[[email protected]@]2(CN3CCC2CC3)O1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

CevimelineAF102BmAChRMuscarinic acetylcholine receptorQuinuclidinexerostomiasialogoguelong-actingsalivationsecretionmuscarinicparasympathomimeticdrymouthInhibitorinhibitorinhibit

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Cevimeline
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HY-70020
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