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Addition of two equivalent amounts of appropriate primary amine to the carbon‐carbon double bonds of 1, 2‐dimaleic acid hydrazine(I) in suitable solvents at room temperature of under reflux provided a number of 1, 2‐bis(N‐substituted β‐aspartyl) hydrazines (IIa‐k) in satisfactory yields. In some cases of this reaction, the mono‐aminated intermediates (IIIa‐c) were also isolated.

I The pharmacological activity of N-[2-(2,6-dimethoxyphenoxy) ethyl]-2-(2-methoxyphenoxy) ethanaminium chloride (ACC-7513) was determined in isolated smooth and cardiac muscle and its effect on blood pressure and heart rate assessed in the spontaneously hypertensive rat (SHR). 2 ACC-7513 was found to be a potent a-adrenoceptor blocking agent (pA2: 8.33) and a 5-hydroxytryptamine (5-HT) antagonist (pA2:7.01), both in rabbit aortic strips. The affinity for aadrenoceptors was about 20 times greater than that for 5-HT-receptors.3 High concentrations of ACC-7513 did not block histamine in rabbit aortic strips, or 13,-or P2-adrenoceptor responses induced by isoprenaline in guinea-pig right atria and trachea, respectively, but did block cholinoceptor responses induced by carbachol in rat uterus, non-competitively. 4 High concentrations of ACC-7513 also produced sino-atrial depression in guinea-pig right atria and direct relaxation of depolarized rabbit aortic strips. 5 ACC-7513 depressed blood pressure of conscious SHRs and produced a reflex increase in heart rate. The reductions in pressure were modest and of short duration. 6 It is concluded that: (a) ACC-7513 is a potent, selective a-adrenoceptor and 5-HT receptor antagonist; and (b) ACC-7513 is not likely to be useful in the treatment of hypertension.

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Cyclopentadien (II) ergibt in 83%iger Ausbeute ein Gemisch aus dem 2‐ und 3‐Substitutionsprodukt (III), das mit Azodicarbonsäurediethylester ein 1:1‐Gemisch der Cycloaddukte (IV) und (V) liefert.