Can CT features be used to diagnose surgical adult bowel intussusceptions?

OBJECTIVE: The purpose of our study was to identify whether any CT characteristics can be used to diagnose surgical intussusceptions. MATERIALS AND METHODS: A search of CT reports on adults revealed 118 patients with 136 intussusceptions. Two blinded readers independently reviewed the CT examinations and documented intussusception characteristics. Medical records were reviewed to determine patient outcome. Performance, interobserver agreement (A), and significance of CT characteristics to identify surgical intussusceptions were calculated. RESULTS: Of 95,223 CT examinations, 0.13% (121/95,223) documented 136 intussusceptions over a 7-year period, of which 88.2% (120/136) were enteroenteric, 3.7% (5/136) were enterocolic, and 4.4% (6/136) were colocolic lesions or in other locations. Eight (5.9%) were surgical and 128 (94.12%) were nonsurgical lesions. Five of eight (63%) surgical lesions involved the colon. Only two of eight surgical lesions had malignant lead points. The mean sensitivity, specificity, positive predictive value, and negative predictive value for diagnosing surgical enteroenteric lesions using a measured lesion length of > 3.5 cm were 100%, 57.3%, 5.7%, and 100% (A = 0.68), respectively. Similar figures using the measured axial diameter > 3 cm were 100%, 32.9%, 3.7% and 100% (A= 0.65), respectively. CONCLUSION: Surgical intussusceptions in adults are infrequent among the intussusceptions that are detected on CT. Most enteroenteric lesions are nonsurgical lesions, whereas lesions that affect the colon are often surgical. Many nonsurgical enteroenteric intussusceptions are longer than 3.5 cm and thicker than 3 cm, suggesting these CT features may not be useful for diagnosing surgical bowel intussusceptions in adults.

Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist.

Indolic N-benzylation of naltrindole reportedly extends the duration of delta-opioid receptor (DOR) antagonism. Similar modification of the kappa-opioid receptor (KOR) antagonist norBNI (1a) and its 17,17'-diNMe analogue (1d), a low potency mu-opioid receptor (MOR) partial agonist, was found to affect predominantly their MOR activity. When administered systemically in mouse antinociceptive assays, N-benzyl-norBNI (1b) had only MOR agonist activity of relatively short duration whereas on central administration it had only a KOR-antagonist action of extremely long duration.

Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.

Derivatives of the highly selective kappa-opioid receptor antagonist GNTI (2a) have been prepared. Binding and functional studies conducted on cloned human opioid receptors expressed in Chinese hamster ovarian (CHO) cells suggested that adding a benzyl or a substituted benzyl group to the guanidino moiety led, in general, to a retention of high kappa-affinity and antagonist potency. Disubstitution of the guanidino moiety led to reduced kappa-selectivity.

Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan.

The effect of substitution of the pyrrolo- and indolo-N atoms in tetrahydronaltrindole (TNTI), tetrahydrooxymorphindole (TOMI), and 17-cyclopropylmethyl-3,14-dihydroxy-4,5-epoxy-4'-phenyl-6,7:2',3'-pyrrolomorphinan (4) is reported. In opioid functional assays 4 were potent deltaopioid receptor (DOR) antagonists while the TNTI derivatives (7) were potent DOR antagonists or low-efficacy DOR partial agonists without substantial selectivity. The TOMI derivatives (8) were DOR agonists with significant selectivity. In vivo the DOR antagonist activity of 7d was confirmed, but the predominant agonist effect of 8d was shown to be mu opioid receptor mediated.

4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity.

A new method for the preparation of N-benzylpyrrolomorphinans has been developed. Thus Michael reaction of the benzylimines of oxycodones and oxymorphones with nitrostyrenes gave a series of 4'-aryl-N-benzylpyrrolomorphinans. These were selective delta antagonists of much higher in vitro potency (with 5a having K(e) delta = <1 nM) than their binding affinities predicted. In mice in vivo assays 5a showed good delta antagonist activity in the anti-writhing analgesic assay and also inhibited delta agonist-induced convulsant activity.