Benzcyclane fumarate  (Synonyms: Bencyclane fumarate; Benzcyclan fumarate)

Benzcyclane fumarate (Bencyclane fumarate; Benzcyclan fumarate) is a serotonin receptor antagonist and a cerebral/peripheral vasodilator. Benzcyclane fumarate exerts atypical serotonin antagonistic effects in rabbit superior mesenteric arteries. Benzcyclane fumarate relaxes high K⁺-induced contractions in rabbit basilar arteries and superior mesenteric arteries, and selectively inhibits sympathetic nerve stimulation-induced contractions in rabbit pulmonary arteries. Benzcyclane fumarate exerts non-competitive norepinephrine antagonistic effects in rabbit superior mesenteric arteries, and slightly reduces the maximum contractile response induced by histamine. Benzcyclane fumarate relaxes smooth muscles, induces transient hypotension, inhibits thrombosis, and accelerates blood fibrinolytic activity. Benzcyclane fumarate increases cerebral glucose content/uptake, enhances hypoxia tolerance in mice, and increases cerebral blood supply in dogs. Benzcyclane fumarate is applicable to studies related to cerebral vascular circulation^[1].

Benzcyclane (0.0001-0.03 mg/mL; 2-3 minutes per concentration, 10-20 minutes for maximum relaxation) fumarate potently relaxes high K⁺-induced contractures in isolated rabbit basilar artery strips with an ED₅₀ of 0.0011 mg/mL, producing faster and more marked relaxation than in mesenteric artery strips^[1].
Benzcyclane fumarate (~30 minutes for maximum relaxation) relaxes high K⁺-induced contractures in isolated rabbit superior mesenteric artery strips with an ED₅₀ of 0.0048 mg/mL, showing weaker and slower relaxation than in basilar artery strips^[1].
Benzcyclane fumarate exerts the strongest antagonistic effect on serotonin-induced contractions in isolated rabbit superior mesenteric artery strips (presumptive pA₂ = 7.3), with weaker noncompetitive antagonism of noradrenaline (pD₂' = 4.3) and minimal effect on histamine (pD₂' = 3.8)^[1].
Benzcyclane (0.006 mg/mL, 0.01 mg/mL; 30 minutes for nerve stimulation, 20 minutes for noradrenaline) fumarate selectively inhibits 25 Hz sympathetic nerve-induced contractions in isolated rabbit pulmonary artery radial muscle preparations without affecting responses to exogenous noradrenaline^[1].

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

405.53

C₂₃H₃₅NO₅

14286-84-1

CN(C)CCCOC1(CC2=CC=CC=C2)CCCCCC1.O=C(O)/C=C/C(O)=O

Room temperature in continental US; may vary elsewhere.

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• [1]. Egawa M, et al. Comparative studies of cerebral vasodilators on relaxation activities in isolated basilar, mesenteric and pulmonary arteries of rabbits. Jpn J Pharmacol. 1982 Apr;32(2):273-81.  [Content Brief]