Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists

The resolution of three 2-substituted derivatives of idazoxan is described. The enantiomers show large separations in activity in a variety of in vitro and in vivo tests, and the active isomers are all potent and selective antagonists at the alpha 2-adrenoreceptor. The significance of these results in relation to those published on the enantiomers of idazoxan and to those on optically active alpha 2-adrenoreceptor agonists is discussed.     

Synthesis of estradiol haptens

Synthesis of Estradiol Haptens Two estradiol haptens, 4-(3β,17β-dihydroxyestran-7α-yl)butanoic acid ( 9 ) and 7α-(4-aminobutyl)-3β,17β-estradiols ( 13 ), were prepared from 19-nortestosterone by partial synthesis. The binding activity for the cytosol estrogen receptor was determined by competition against [³H]-estradiol; at a concentration of 2×10^?7mol/l, compound 9 displaces 50% of [³H]-estradiol. Attached to AH-Sepharose 4B compound 9 allows the cytosol estrogen receptor from calf uterus to be concentrated 1800-fold by affinity chromatography.     

Suppression of rotavirus SA-11 reproduction by protease inhibitors in cell culture

The effect of proteases inhibitors, epsilon-amino-caproic acid and gordox, on reproduction of rotavirus SA-11 in MA-104 cells was studied by enzyme immunoassay. These inhibitors were shown to exert an inhibiting effect on rotavirus reproduction.     

Effect of gradual rise in plasma calcium concentration on the impairment of atrioventricular nodal conduction due to verapamil

The possible reversal by calcium of the inhibitory action of verapamil on the atrioventricular (AV) node was investigated in anesthetized, atropinized dogs, with cardiac pacing. The His bundle potentials were recorded by endocavitory electrode and the AV node effective refractory period measured by the extrastimulus method. Calcium infusion was effective against the impairment of AV nodal conduction induced by verapamil, provided it remained moderate: the gradual rise in the plasma calcium concentration counteracted the effects of an infusion of verapamil on conduction time and effective refractory period in the AV node, as long as it did not exceed 5 mmol/L. However, beyond this level, calcium appeared less and less capable of reversing the effects of verapamil. Thus, the protective action of calcium had a bell-shaped dose-response curve, with the optimum at 5 mmol/L. This biphasic influence is consistent with the opposite opinions previously given concerning the antagonism between calcium and calcium blockers, depending on whether hypercalcemia brought into play was mild or major. In any case, the prominent role played by calcium in the slow inward current in the AV node accounts for the antagonism, observed in vivo, between calcium and verapamil. The pacemaker activity of the sinoatrial (SA) node was less influenced by both calcium blocker and calcium.     

Immunogenicity of Haemophilus influenzae type b capsular polysaccharide vaccines in 18-month-old infants

Haemophilus influenzae vaccine containing polyribosyl ribitol phosphate (PRP) or PRP covalently linked to diphtheria toxoid (PRP-D) was given to 94 healthy infants 17 to 22 months of age at the same time, but not at the same site, as a diphtheria-tetanus-pertussis booster. Systemic reactions were similar in the two vaccine groups and resembled those expected with the diphtheria-tetanus-pertussis injection alone. Six (13%) and seven (14%) of the PRP and PRP-D recipients, respectively, had minor local reactions to the Haemophilus vaccine. Among the 77 children who were not already naturally immune (ie, anti-PRP antibody concentration of less than or equal to 0.15 micrograms of protein per milliliter) before vaccination, PRP-D was significantly more effective than PRP in inducing protective levels of antibody. Only 15 (43%) of the 35 nonimmune PRP recipients achieved a concentration of greater than or equal to 0.15 microgram/mL and only seven (20%) reached a concentration greater than or equal to 1.0 micrograms/mL following vaccination. In contrast, 34 (81%) of the 42 nonimmune recipients of PRP-D had a concentration of greater than or equal to 0.15 microgram/mL following vaccine and 32 (62%) had a concentration of greater than or equal to 1.0 micrograms/mL (P less than or equal to .001). These results suggest that more than one-half of nonimmune 18-month-old infants will not respond to PRP with protective levels of antibody. In light of the current data, recommendation for revaccination at 24 months of age for those immunized at any younger age is appropriate.     

A review of professional liability cases affecting the practice of optometry

In establishing the liability of optometrists for negligence the courts have applied the same standard of care that is imposed upon other health care professionals, holding that optometrists must employ the minimum degree of skill, care and learning that is ordinarily exhibited by members of the profession who are in good standing. The leading cases establishing this standard have involved glaucoma, retinal detachment, and intraocular tumors. Optometrists have also been held liable under product liability law for injuries caused by ophthalmic lenses, which illustrates the trend toward strict liability. Other cases have involved the doctrine of informed consent.     

Movement timing in deaf and hearing speakers: comparison of phonetically heterogeneous syllable strings

We review evidence suggesting that deaf speakers do not move their articulators toward the following open posture throughout closure and report results from a preliminary cinefluorographic study. Two prelingually deaf and two hearing speakers produced two different strings of alternating heterogeneous monosyllables as though speaking in time with a metronome (the so-called P-center task). Events traditionally associated with vowel production appeared evenly timed throughout the productions, and, in general, the deaf speakers performed similarly to the hearing speakers. We relate the results to Fowler's (1983) interpretation of the P-center phenomenon as an indicant of continuous vowel production.