A novel electrosynthetic system for anodic substitution reactions by using parallel laminar flow in a microflow reactor.

We have developed a novel electrosynthetic system for anodic substitution reactions by using parallel laminar flow in a microflow reactor. This system enables nucleophilic reactions to overcome the restraint, such as the oxidation potential of nucleophiles and the stability of cationic intermediates, by the combined use of ionic liquids as reaction media and the parallel laminar flow in the microflow reactor. By using this novel electrosynthetic system, the anodic substitution reaction of carbamates, especially of cyclic carbamates, with allyltrimethylsilane were carried out to provide the corresponding products in moderate to good conversion yields in a single flow-through operation at ambient temperature (without the need for low-temperature conditions).

NMR structural study of two-disulfide variant of hen lysozyme: 2SS[6-127, 30-115]--a disulfide intermediate with a partly unfolded structure.

The 15N-labeled recombinant hen lysozyme and two species of two-disulfide variants, denoted as 2SS[6-127, 30-115] and 2SS[64-80, 76-94], were studied by means of NMR spectroscopy. The former variant contains two disulfide bridges in the alpha-domain, while the latter has one disulfide bridge in the beta-domain and the other one at the interface between two domains. Resonance assignments were performed using 3D TOCSY-HSQC and NOESY-HSQC spectra.

General pharmacological properties of the human corticotropin-releasing hormone corticorelin (human).

General pharmacological effects of the human corticotropin-releasing hormone, corticorelin (human) (CAS 86784-80-7), on the central nervous system, somatic nervous system, autonomic nervous system and smooth muscle, respiratory and circulatory system, digestive system and miscellaneous organs were investigated. 1. The central nervous system: Corticorelin (human) had little effect on hexobarbital-induced sleeping-time, maximal electroshock-induced convulsion, acetic acid-induced writhing, rota-rod performance.

[Effects of terazosin on the blood pressure responses to tilting in conscious animals: comparison with prazosin].

Inhibitory effects of terazosin on the compensatory blood pressure responses to tilting were studied in conscious rabbits and spontaneously hypertensive rats (SHR). In rabbits, doses which reduced the mean blood pressure by 15 mmHg were 330 micrograms/kg, i.v.

Effect of MCI-176, a new calcium antagonist, on the calcium induced contraction of isolated porcine coronary arteries.

Calcium antagonistic activity of MCI-176, a new calcium antagonist, was compared with those of diltiazem and nifedipine in isolated depolarized porcine coronary arteries. MCI-176, diltiazem and nifedipine competitively inhibited calcium contraction of the large coronary arteries, and their pA2 values were 7.49, 6.

[Alpha-adrenoceptor blocking action of terazosin].

alpha-Adrenoceptor blocking activities and vascular relaxation activities of terazosin, a new antihypertensive agent, were studied. Terazosin had no effect on Ba2+, serotonin, angiotensin II and Ca2+ induced contractions in the isolated rat aorta. Terazosin competitively inhibited norepinephrine (NE) and phenylephrine (PE) induced contractions of the isolated rat aorta, and their pA2 values were 9.

Coronary dilator effect of MCI-176, a new calcium channel blocker, in dogs.

Effects of MCI-176, 2-(2,5-dimethoxyphenylmethyl)-3-(2-dimethylaminoethyl)-6-isopropox y-4 (3H)-quinazolinone hydrochloride, on coronary and aortic blood flows, mean blood pressure and heart rate were investigated in comparison with those of diltiazem in anesthetized dogs. MCI-176, like diltiazem, dose-dependently increased coronary and aortic blood flows and decreased mean blood pressure. In producing these effect MCI-176 was slightly but significantly more potent than diltiazem.

[Cardiovascular effects of MY-5116 and MY-1250].

The effects of MY-5116, isoamyl 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c]quinoline-2-carboxylate, an anti-allergic drug, and MY-1250, an active metabolite of MY-5116, on the cardiovascular system were studied in dogs, rats and guinea pigs. Orally administered MY-5116 (300 mg/kg) had no effect on the cardiovascular system in anesthetized dogs and conscious rats. In anesthetized dogs, MY-1250 and disodium cromoglycate (DSCG) caused hypotension, bradycardia and reduction of respiration rate from the doses of 3 and 10 micrograms/kg, i.

A device for indirect measurement of blood pressure in conscious dogs.

A technique for indirect measurement of blood pressure by a combination of commercially available apparatuses was devised. There were good correlations in both of systolic and diastolic blood pressures measured by the indirect and direct methods.

[Effect of suloctidil on the contractions of isolated rat aortic strips induced by norepinephrine and CaCl2].

The mode for the antispasmodic action of suloctidil was examined using aorta strips of rats in vitro. Both 10 microM suloctidil and 0.1 microM verapamil non-competitively inhibited the norepinephrine (NE)-induced contraction, of which pD'2 values were 4.

[Effect of suloctidil on the dynamics of the peripheral artery of the dog].

The effects of suloctidil, an antispasmodic agent, on the femoral, renal, superior mesenteric, common carotid and vertebral blood flows were compared with those of papaverine and cinnarizine using electromagnetic flow meters in pentobarbital anesthetized dogs. In i.v.

[Effect of suloctidil on cerebral venous outflow in the dog (author's transl)].

The effects of intravenous administration of suloctidil [erythro-1-(4-isopropylthiophenyl)-2-n-octylamino-propanol], (MY 103) on cerebral venous outflow (VOF), blood gases, cerebral metabolic rate of oxygen (CMRO2) and other hemodynamic parameters were studied and effects compared to those of cinnarizine and papaverine, in gallamine immobilized dogs. MY103 and papaverine at doses 0.1-1.

Vasodilation produced by prostacyclin (PGI2) and 9(O)-thiaprostacyclin (PGI2-S) in the canine femoral circulation.

The action of 9(0)-thiaprostacyclin (PGI2-S) was compared with that of prostacyclin (PGI2) and papaverine in the femoral circulation of dogs. PGI2-S, injected into the dog femoral artery in a dose of 0.1 microgram or higher, produced marked vasodilation in the femoral artery without any change in blood pressure.

Effects of ethyl adenosine-5'-carboxylate on the heart and coronary circulation.

Using the canine heart-lung preparation supported by a donor, the effects of ehtyl adenosine-5'-carboxylate (EAC) on the heart and coronary circulation were studied and compared with those of adenosine. EAC produced qualitatively similar effects to adenosine in this preparation. Aminophylline inhibited the effects of EAC as well as those of adenosine.