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Summary: The authors investigated the relationship between ejaculation and spinal monoamine levels by transecting the dog spinal cord at the various levels. From the results obtained in this study it was concluded that the lumbar and upper sacral segments of the spinal cord are important for ejaculation, and that the suppression of ejaculation by lower lumbar to upper sacral transection may be induced by increase in serotonin in the Sth lumbar — 1st sacral segments. Zusammenfassung: Die Autoren untersuchten Zusammenhange zwischen Ejakulation und spinalen Monoaminkonzentrationen nach Durchtrennung der Ruckenmarksbahnen in verschiedenen Segmenten beim Hund. Aus den Ergebnissen dieser Studie ist zu schliesen, das die Segmente des Lumbal- und oberen Sacralmarks fur die Ejakulation von Bedeutung sind, und das die Unterdruckung der Ejakulation nach Durchtrennen des unteren Lumbal-bis zum oberen Sacralmark induziert sein konnte durch einen Anstieg des Serotonins im 5. Lumbal- und 1. Sacralsegment.

A high-performance liquid chromatography (HPLC) procedure was developed for the determination of plasma gliclazide, a new oral hypoglycemic drug. Gliclazide, tolbutamide (used as an internal standard) and plasma components in plasma were successfully separated as sharp peaks by reversed-phase HPLC on a Jasco SC-01 column with methyl alcohol containing 0.2% acetic acid (3 : 2, v/v) as the mobile phase (retention time ; gliclazide : 16 min, IS : 10 min, plasma components : 5.5 and 7.0 min). The relationship between the plasma levels of gliclazide and the peak height ratio (gliclazide/IS) was linear (correlation coefficient, γ=1.00) in the range of 0.3 to 10 μg/ml plasma. The detection limit and the reproducibility (CV) of the present method were 0.3μg/ml and 4.0% (n=8), respectively. The decay curve of plasma gliclazide in a diabetic patient given 80 mg of the drug orally was determined by the present method and GLC (ECD method). The two results agreed well. Reversed-phase HPLC was shown to be suitable for the routine clinical assay of gliclazide in plasma.

The peripheral nervous pathways controlling seminal emission and closure of the internal urethral orifice during ejaculation were examined experimentally using male adolescent dogs. The experimental methods were measurement of the contraction of the internal urethral orifice and measurement of the change of the posterior urethral pressure induced by selective stimulation of the nerves related to the hypogastric nerve. Further, the change of actual ejaculation caused by manual stimulation of the penis was observed after excision of the nerves. Results included the following: (1) The seminal emission and the closure of the internal urethral orifice on ejaculation were controlled by the hypogastric nerve. (2) The nerve fibers which controlled these two phenomena took different paths above the lower mesenteric plexus. (3) Seminal emission was controlled by the splanchnic nerves which originated from the lower thoracic and upper lumbar ganglia of the sympathetic trunk, and the closure of the internal urethral orifice by those which originated from the lower lumbar ganglia of the trunk.

Many alkyl 4-(2-oxo-1, 2, 3, 4-tetrahydro-6-quinolyloxy) butyrates and related compounds were synthesized and tested for inhibitory activity against blood platelet aggregation in vitro. Among them, ethyl 4-(2-oxo-1, 2, 3, 4-tetrahydro-6-quinolyloxy) butyrate was found to have the most potent inhibitory activity. The structure-activity relationships are discussed.

The effects of 5-HTP and pCPA on manually induced ejaculation in dogs and on brain monoamines in dogs and rats were investigated. From the results obtained in this study it was concluded that the serotonergic system in the brain is the mechanism which inhibits the occurrence of ejaculation. Considered together with the results obtained in our previous paper, it is though that ejaculation occurs with the reconciliation of the dopaminergic and serotonergic systems.

The acylase activity of a strain (KT 218) of soil bacteria was tested against N-benzoyl and N-dichloroacetyl derivatives of 2-aminooctanoic, 2-aminodecanoic, 2-aminolauric, 2-aminomyristic, and 2-aminopalmitic acid. It was revealed that the dichloroacetylaminoacids were more easily hydrolyzed than the corresponding benzoylamino acids and that the N-dichloroacetyl-derivatives of the homologous series of straight chain 2-aminoacid were hydrolyzed at progressively decreasing rates from N-dichloroacetyl-DL-2-aminooctanoic acid to N-dichloroacetyl-DL-2-aminopalmitic acid which was resistant to KT 218 acylase.The acetone powder of KT 218 effected asymmetric hydrolysis of N-dichloroacetyl derivatives of 2-aminooctanoic, 2-aminodecanoic, 2-aminolauric, 2-aminomyristic acids to yield respectively L-2-aminooctanoic acid (XI) and N-dichloroacetyl-D-2-aminooctanoic acid (XV), L-2-aminodecanoic acid (XII) and N-dichloroacetyl-D-2-aminodecanoic acid (XVI), L-2-aminolauric acid (XIII) and N-dichloroacetyl-D-2-aminolauric acid (XVII), and L-2-aminomyristic acid (XIV) and impure N-dichloroacetyl-D-2-aminomyristic acid. In the same way KT 218 acetone powder effected asymmetric hydrolysis of N-benzoyl derivatives of 2-aminooctanoic, 2-aminodecanoic, and 2-aminolauric acids to yield respectively L-2-aminooctanoic acid (XI) and N-benzoyl-D-2-aminooctanoic acid (XVIII), L-2-aminodecanoic acid (XII) and impure N-benzoyl-D-2-aminodecanoic acid, and L-2-aminolauric acid (XIII) and impure N-benzoyl-D-2-aminolauric acid.

Erection and ejaculation were caused in male mongrel dogs by manual stimulation of the penis and the pressure changes in the posterior urethra during this stimulation were recorded. As a result, it was noted that the pressure changes in the posterior urethra from the onset of the stimulation to the end of ejaculation were identical to those seen in the posterior urethrogram reported in the previous paper, and that rhythmic alterations in the posterior urethrogram coincided with the pressure change in the posterior urethra during actual ejaculation.

SINCE Kogl and Erxleben showed, in 1939, that D-glutamic acid can be isolated from cancerous tissue, D-peptidases have been the subject of many researches. Kogl and Erxleben's demonstration seems to have particular interest, when considered together with the fact that penicillins, on acid hydrolysis, yield an amino-acid of D-configuration, penicillamine, on one hand, and the fact that both antibiotics, tyrocidin and gramicidin S, give D-phenylalanine as their hydrolysis product, on the other. While engaged in the study of capability of soil bacteria to metabolize benzoic acid and its related compounds, and some amino-acids1, we have recently observed that, of thirty-four strains of soil bacteria employed in our experiment, two strains, KT82 and KT83, have the ability to utilize benzoyl-D-phenylalanine (melting point 139°–140°; [α]D13= − 14.9) as well as benzoyl-L-phenylalanine (melting point 139°–140°; [α]D13= + 14.8) as the sole source of carbon and nitrogen.

WHILE engaged in the study of metabolism and hydrolysis by soil bacteria of benzoic acid derivatives, amino-acids, and acylated amino-acids1–4, we noticed that soil bacteria KT 231 and KT 233 have the metabolic activity shown in Table 1. The constituents of the culture medium used in the experiments were as follows: NH4Cl, 0.1 gm.; K2HPO4, 0.1 gm.; MgSO4.7H2O, 0.05 gm.; 1 per cent CaCl2.6H2O, 2 drops; 1 per cent FeCl3.6H2O, 1 drop; organic substance to be tested, 0.2 gm.; distilled water, 100 ml.; pH 7.4–7.6 (adjusted with 10 per cent sodium hydroxide).

The post-surgical effects of ureterostomy and nephrostomy were compared, and the following results were obtained: (1) reduction of renal function was greater after ureterostomy than after nephrostomy and (2) pyelonephritis occurred more frequently following ureterostomy than nephrostomy. In addition, electoureterography and urometrography were conducted in 10 cases following ureterostomy. One case of them showed normal ureteral peristalsis, 4 cases showed irregular peristalsis, and in the remaining 5 cases peristalsis failed to occur.

Fifteen strains (KT 202, KT 205, KT 207, etc.) of soil bacteria capable of asymmetric hydrolysis of N-benzoyl-DL-threonine, 2, 6-di-N-benzoyl-DL-lysine, N-acetyl-DLlysine, N-acetyl-DL-tryptophan or N-acetyl-DL-methionine were isolated by using a synthetic medium containing N-acyl-derivatives of amino acids as the sole source of carbon (Table I).N-Benzoyl-DL-threonine was asymmetrically hydrolyzed to L-threonine, N-benzoyl-D-threonine and benzoic acid by the acylase of KT 218, KT 229, and KT 83, while 2, 6-di-N-benzoyl-DL-lysine, to 6-N-benzoyl-L-lysine, 2, 6-di-N-benzoyl-D-lysine and benzoic acid by KT 218 and KT 229.KT 241 and KT 224 hydrolyzed asymmetrically N- acetyl- DL-tryptophan and N-acetyl-DL-methionine to L-tryptophan and N-acetyl-D-tryptophan, and L-methionine and N-acetyl-D-methionine, respectively.It was observed that N-acetyl-D-tryptophan and N-acetyl-D-methionine were hydrolyzed by several strains (KT 229, KT 83, KT 222, etc.) of soil bacteria.It seems of interest to note that N-acetyl-L-methionine was more easily hydrolyzed by KT 224 or KT 218 than N-acetyl-L-tryptophan, while the latter was more easily hydrolyzed by KT 241, and that the N-acetyl derivative of L-methionine was more easily hydrolyzed by KT 224 or KT 241 than the N-benzoyl derivative, while the latter was more easily hydrolyzed by KT 218.

The effects of autonomic drugs on seminal emission and ejaculation were investigated in mongrel dogs. Changes in the posterior urethral pressure (posterior urethrogram) and the volume of seminal emission during continuous hypogastric nerve stimulation were measured in test animals. The seminal emission induced by hypogastric nerve stimulation caused continuous rise in the posterior urethral pressure. When the pressure reached the maximum level, rhythmic alterations of the pressure which was considered, to be a phenomenon associated with ejaculation occurred. The drugs were administered into the abdominal aorta just above its bifurcation. Tetrodotoxin (1-5 μg) abolished both seminal emission and rhythmic alterations of the posterior urethral pressure. Phenylephrine (10-100 μg) and methoxamine (10-30 μg) increased markedly the seminal emission and induced the rhythmic alterations. Phentolamine (1-10mg) and phenoxybenzamine (1-10mg) abolished both seminal emission and the rhythmic alterations. Administration of isoproterenol (10-30 μg) or propranolol (1-10mg) affected neither seminal emission nor rhythmic alterations. Acetyl-choline (1-10 μg) or atropine (1-10 μg) did not show any definite effect on both seminal emission and the rhythmic alterations. No significant effect of DMPP (10-30 μg) on seminal emission and rhythmic alterations were observed. No significant change in seminal emission was caused by hexamethonium (100-500 μg). The rhythmic alterations were not affected by this agent in many dogs. From these results it is concluded that both seminal emission and ejaculation are predominantly under the influence of adrenergic nervous system, particularly through an a-adrenergic receptor mechanism

Ureteral activity during the intravesical infusion was examined by urometry and electro-ureterograpby in 12 normal persons and a patient with vesico-ureteral reflux. The urometrograms and electro-ureterograms in normal persons indicated that when the bladder was distended with physiologic saline solution, the ureteral peristalsis responded so as to overcome the increased intravosical pressure. In the case with vesico-ureteral reflux, the ureteral peristalsis was found to be preserved. The values measured on the urometrogram and electro-ureterogram were all within the range of normal ones, and the urine was transported smoothly from the renal pelvis to the bladder without the reflux, when the intravesical pressure was below 10cm H2O. When the intravesical pressure was raised up to 10cm H2O, the reflux appeared. Even in this ureter persitalsis responded so as to flow out the refluxed urine. These findings suggest that ureteral perisitalis, if it remains, works to repress the veiico-ureteral reflux as far as it can resist the increased intravesical pressure and that it works against the reflux, when it actually occurs.

IN work reported earlier1, it was shown that a strain of Pseudomonas sp., KT83, can hydrolyse N-benzoyl derivatives of both L- and D-forms of amino-acids such as phenylalanine, tyrosine and alanine.

The variations of serum potassium and of total exchangeable potassium (T. E. potassium) were examined before and after the operations on 75 urological patients: 50 aged patients and, as control subjects, 25 young patients. In the control group, serum potassium was always within the normal range throughout the course, while slight reduction in T. E. potassium level occurred in 1 to 2 weeks postoperatively. In the aged group, serum potassium was almost within the normal range before the operation, but it decreased markedly after the operation and the decreased state lasted for a week in many cases, or louger in some cases. T. E. potassium in the aged group was within normal range in many cases, although a fall below the normal range was revealed in some cases. In almost all cases a tendency for the T. E. potassium to lower below normal range was recognized 1 to 2 weeks after the operation. T. E. potassium did not recover the preoperative value 3 to 5 weeks later. Correlation between serum potassium and T. E. potassium was examined both in the young and aged groups. In the young group, serum potassium and T. E. potassium levels were well correlated in both pre- and postoperative periods. In the aged group, many cases showed a correlation between the two values in preoperative period but no correlation was revealed in the postoperative period, due to reduction of T. E. potassium level. Three to 5 weeks after the operation, serum potassium level lowered to some degree, showing a correlated state below the normal range of both serum and T. E. potassium levels. Eight to 10 weeks later, both potassium levels began to rise and the correlation was reestablished within the normal range.

IN a previous communication1 we have reported that two strains (KT 83 and KT 82) of soil bacteria were able to utilize benzoyl-D-phenylalanine as well as benzoyl-L-phenylalanine as a sole source of carbon and nitrogen, whereas one strain (KT 84) could utilize the L-form but not the D-form, and that benzoyl-D-phenylalanine was hydrolysed by a suspension of either KT 83 or KT 82, but not by KT 84.

BATCHELOR et al. discussed the isolation of 6-aminopenicillanic acid (I) from a submerged culture of Penicillium chrysogenum1. Recently, it was shown that (I) could be prepared by the microbial hydrolysis of benzylpenicillin (II)2–4.

WHILE investigating the specificity of acylase activity of soil bacteria on acyl derivatives of aminoacids1–3, we noted that the acetone powder of Ehrlich ascites carcinoma cells was able to hydrolyse dichloro-acetyl-DL-aspartic acid but not (or only to a small extent) the dichloroacetyl derivatives of some aminoacids such as DL-glutamic acid, DL-serine, DL-methionine and DL-phenylalanine4.