van Zwieten P A, Timmermans P B
Pharmacology. 1980;21(5):327-32. doi: 10.1159/000137448.
The acute hypotensive and bradycardic effects of the new compound B-HT 933 (2-amino-6-ethyl-4,5,7,8-tetrahydro-6H-oxazolo-[5,4-d]-azepin-dihydrochloride) were investigated in anaesthetized cats and rats. In spite of the molecular structure of B-HT 933, which differs considerably from that of clonidine, its cardiovascular reaction pattern is comparable, although the former is much less potent. B-HT 933 showed a central nervous origin for its acute hypotensive action in anaesthetized cats, since its effects on blood pressure after infusion via the left vertebral artery were much greater than after intravenous application of the same amounts. Pretreatment with the alpha-adrenoceptor-blocking drug, piperoxan (100 micrograms/kg), completely abolished the hypotensive response to B-HT 933 (30 micrograms/kg) injected subsequently via the left vertebral artery. It is concluded that B-HT 933 is a centrally acting hypotensive drug. Central alpha-adrenoceptors are involved in a similar manner as the mechanism of clonidine.
研究了新型化合物B-HT 933（2-氨基-6-乙基-4,5,7,8-四氢-6H-恶唑并-[5,4-d]-氮杂卓二盐酸盐）对麻醉猫和大鼠的急性降压和减慢心率作用。尽管B-HT 933的分子结构与可乐定有很大不同，但其心血管反应模式相似，尽管前者的效力要低得多。在麻醉猫中，B-HT 933的急性降压作用显示出中枢神经起源，因为经左椎动脉输注后其对血压的影响远大于静脉注射相同剂量后的影响。用α-肾上腺素受体阻断药哌罗克生（100微克/千克）预处理，可完全消除随后经左椎动脉注射B-HT 933（30微克/千克）引起的降压反应。结论是B-HT 933是一种中枢性降压药。中枢α-肾上腺素受体的参与方式与可乐定的机制相似。
