BTM-1086 

BTM-1086 is a potent anti-ulcer and gastric secretory inhibiting agent.

Muscarinic receptor^[1]

Functional and binding experiments shows that the (-) enantiomer (BTM-1086) has a high affinity (pK_i=8.31-9.15) for the three muscarinic receptor subtypes in guinea-pig cortex (M1), heart (M2) and salivary glands (M3)^[1].

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

BTM-1086 prevents the development of ulcer at a dose of 0.1 to 1 mg/kg, p.o., but only weakly inhibits the histamine induced gastric ulcer. The inhibitory activities of BTM-1086 are significantly higher than those of atropine sulfate. In the healing experiment with the acetic acid-induced stomach ulcer, BTM-1086 (1 mg/kg/day , p.o., x14) shows a significant healing effect, which is higher than that of propantheline bromide . BTM-1086 at a dose of 0.2 mg/kg , i.d., remarkably inhibits the gastric secretion 6 hr after pylorus ligation. The aspirin-induced reductions of the total acid and K⁺ as well as the increments of the volume and Na⁺ in the gastric secretion are prevented dose-dependently by pretreatment with BTM-1086. The LD₅₀ value by oral, s.c., and i.v. administration with this compound is 880, 630 and 113 mg/kg, respectively, for male rats and 830, 650 and 119 mg/kg, respectively, for female rats^[2].

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

367.51

C₂₁H₂₅N₃OS

72293-17-5

O=C1[C@H](CN2CCN(C)CC2)[C@H](C3=CC=CC=C3)SC4=CC=CC=C4N1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Eltze M, et al. Affinity profiles of BTM-1086 and BTM-1041 at muscarinic receptor subtypes and at H1- and alpha 1-receptors. Eur J Pharmacol. 1989 Nov 7;170(3):225-34.  [Content Brief]

  [2]. Hajimu Y, et al. Antiulcer Effect of (-)-cis-2, 3-Dihydro-3-(4-Methylpiperazinylmethyl)-2-Phenyl-1, 5-Benzothiazepin-4-(5H)-One Hydrochloride (BTM-1086) in Experimental Animals. Japan J Pharmacol. 41, 283-292 (1986).