Methiothepin maleate  (Synonyms: Metitepine maleate; Ro-8-6837 maleate)

Methiothepin maleate is a potent and non-selective 5-HT₂ receptor antagonist, with pK_ds of 7.10 (5-HT_1A), 7.28 (5HT_1B), 7.56 (5HT_1C), 6.99 (5HT_1D), 7.0 (5-HT_5A), 7.8 (5-HT_5B), 8.74 (5-HT₆), and 8.99 (5-HT₇), and pK_is of 8.50 (5HT_2A), 8.68 (5HT_2B), and 8.35 (5HT_2C).

pKd: 7.10 (5-HT_1A), 7.28 (5HT_1B), 7.56 (5HT_1C), 6.99 (5HT_1D)^[1], 7.0 (5-HT_5A), 7.8 (5-HT_5B), 8.74 (5-HT₆), 8.99 (5-HT₇)^[3]
pKi: 8.50 (5-HT_2A), 8.68 (5-HT_2B), 8.35 (5-HT_2C)^[2]

Methiothepin maleate is a 5-HT receptor antagonist, with pK_ds of 7.10, 7.28, 7.56, and 6.99 for 5-HT_1A, 5HT_1B, 5HT_1C, 5HT_1D^[1]. Methiothepin mesylate also shows pK_ds of 7.0, 7.8, 8.74, and 8.99 for 5-HT_5A, 5-HT_5B, 5-HT₆, and 5-HT₇, respectively^[2]. Methiothepin exhibits high affinity at 5-HT_2A, 5HT_2B, and 5HT_2C with pK_is of 8.50, 8.68, and 8.35, respectively^[3].

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

472.62

C₂₄H₂₈N₂O₄S₂

19728-88-2

CN1CCN(C2CC3=CC=CC=C3SC4=CC=C(SC)C=C24)CC1.OC(/C=C\C(O)=O)=O

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

• [1]. Schoeffter P, et al. 5-Hydroxytryptamine (5-HT)-induced endothelium-dependent relaxation of pig coronary arteries is mediated by 5-HT receptors similar to the 5-HT1D receptor subtype. J Pharmacol Exp Ther. 1990 Jan;252(1):387-95.  [Content Brief]

  [2]. Knight AR, et al. Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23. Epub 2004 Jul 30.  [Content Brief]

  [3]. Hoyer D, et al. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol Rev. 1994 Jun;46(2):157-203.  [Content Brief]