3-Pyridyl ethers as SPECT radioligands for imaging nicotinic acetylcholine receptors.

To develop a suitable single photon emission computed tomography (SPECT) radioligand for neuronal nicotinic acetylcholine receptors (nAChRs) that displays faster in vivo kinetics than 5-[123I]iodo-A-85380, we synthesised the radioiodinated analogue of A-84543. 5-[123I]Iodo-A-84543 was prepared by electrophilic iododestannylation in a modest yield of 23%. In the baboon brain, 5-[123I]iodo-A-85380 displayed a profile consistent with the known distribution of nAChRs, however, 5-[123I]iodo-A-84543 displayed a homogenous uptake with no preferential localisation in regions known to contain nAChRs. To examine the effect of halogen substitution on the 3-pyridyl ether, A-84543, the 5-chloro, 5-bromo and 5-iodo analogues were synthesised and evaluated with respect to nAChR binding. In vitro binding data revealed that halogen substitution at the 5-position of A-84543 was not well tolerated with an increase in halogen size resulting in lower binding towards nAChRs. The 5-chloro analogue 4 displayed highest affinity, Ki =1.3 nM, compared to the 5-bromo and 5-iodo compounds, 5 Ki =3.3 nM and 3 Ki =40.8 nM, respectively. Taken together, these results clearly indicate that 5-[123I]iodo-A-84543 is not suitable for the study of nAChRs in vivo using SPECT.     

Sarcomas of the Uterus: Morphological Criteria and Clinical Course

Sixty-nine cases of uterine sarcoma were reviewed histologically with respect to their grade of malignancy. Mitotic activity is the most important criterion of malignancy.A histological grading was performed on the basis of mitotic counts per high power field. Clinical follow-up showed that except for the local extension of the tumor, the prognosis of sarcomas depends greatly on mitotic activity. There is a good correlation in the lower stages I and II between number of mitoses and survival rate. The 5 year survival rate of patients with grades I or II is 77% compared to 41% for grades III and IV.Vascular invasion is not evident in distant metastases in our material. Adjuvant chemotherapy is recommended in clinical stages II–IV and in histological grades III and IV.     

Sarcomas of the Female Genitalia: Therapy and Prognosis

216 sarcomas of the female genitalia were treated at the University hospitals for women of Freiburg and Tübingen between the years 1957 to 1977. 76% originated from the uterine corpus; 28% (46/164) of the sarcomas of the corpus uteri were detected as incidental findings. The 5 year survival rate is 54% in stage I, 25% in stage II, and 40% in all stages (52/131). Postoperative irradiation of stage I cases of sarcomas of the corpus uteri diminished local recurrence but not metastases. Extirpation of the ovaries has no influence on local recurrence.Sarcomas of the vulva and cervix have a comparatively good prognosis, whereas the prognosis of the sarcoma of the ovary is very bad.The bad prognosis of sarcomas of the female genitalia points out the necessity of developing cooperative clinical trials on the effectiveness of adjuvant chemotherapy.     

Pancreas divisum: thin-section CT

Twelve patients with known pancreas divisum underwent thin-section computed tomography (CT) to determine the capability of CT to depict this pancreatic anomaly. Focal pancreatic enlargement was present in five patients. Two distinct pancreatic moieties separated by a fat cleft were noted in three patients; a fourth patient had focal atrophy in the distribution of the dorsal pancreas. The two pancreatic moieties were identified at the same craniocaudal level in all four of these patients. The dorsal duct was depicted in all 12 patients, while the short ventral duct was seen in only five of the 12 patients. Failure of the ventral and dorsal pancreatic ducts to fuse was identified in all five patients in whom both ducts were seen. CT may not enable specific diagnosis of pancreas divisum in the majority of patients. If, however, distinct pancreatic moieties or unfused ductal systems are evident, the diagnosis may be confidently suggested.     

Self-limiting extravasation in the unused urinary bladder

Patients being evaluated as potential renal transplant recipients routinely undergo voiding cystourethrography. Eight patients were encountered in whom extraperitoneal extravasation was noted from the region of the ureterovesical junction during voiding (seven patients) or during filling (one patient). Extravasation was bilateral in six patients and unilateral in two. The patients neither experienced symptoms related to the extravasation, required treatment, nor had sequelae. Five of the eight patients have subsequently received renal transplants and their bladders were observed to be normal at surgery. Cystoscopy was also performed in two of these five patients and was unremarkable. After transplantation, these patients' bladders functioned normally and gave rise to no symptoms.     

Plasma amino acid level in rheumatoid arthritis and ankylosing spondylitis and its variation during age

28 plasma amino acids of 40 female patients with rheumatoid arthritis (RA), 24 male patients with ankylosing spondylitis (ASp) and 19 controls (14 females and 5 males) were investigated. In RA-patients 19 amino acids showed statistically significant differences to healthy people of which 18 were decreased. In ASp-patients 14 amino acid concentrations were statistically altered whereby 10 showed enhanced values. In female RA-patients and controls a linear dependency between distinct amino acids (threonine, glutamic acid, proline, alanine, citrulline, tyrosine, phenylalanine, ornithine, lysine and 3-methylhistidine) - and advanced age could be demonstrated.