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Biomedical subjects

J Lear

Publications and source records attributed to J Lear.

34 records · Page 2Linked to original sources
PubMed1994

Crystal and molecular structures of tricyclic neuroleptics.

The X-ray crystal structures of three tricyclic neuroleptics have been completed and are reported herein. These include amitriptyline hydrochloride (I), chlorprothixene hydrochloride (II), and ethopropazine hydrochloride (III). The structures were compared with the structures of similar molecules with similar pharmacological activity. It was found that there is a great deal of flexibility in the structures of these molecules, which makes it difficult to determine the pharmacologically active conformations. Crystallographic data: (I) C20H24NCl, monoclinic space group P2(1)/a, a = 13.812(4) A, b = 9.140(2) A, c = 14.345(4) A, beta = 96.82(2) degrees, Z = 4, final R = 0.059 for 1630 observed (l > 3 sigma(l)) reflections. (II) C18H20NSCl2.CHCl3, monoclinic space group C2/c, a = 29.416(4) A, b = 6.986(1) A, c = 23.374(3) A, beta = 109.78(1) degrees, Z = 8, final R = 0.046 for 1436 observed reflections. (III) C19H25N2SCl, monoclinic space group P2(1)/c, a = 8.849(1) A, b = 14.475(2) A, c = 14.832(1) A, beta = 98.72(1) degrees, Z = 4, final R = 0.039 for 2583 observed reflections.

Antidepressive Agents, Tricyclic↗
PubMed1994

Collapse in an accident and emergency department.

Collapse is a common presenting complaint to accident and emergency (A & E) departments. This retrospective study of 4180 new attendances at a district general hospital A & E showed that this accounted for 2.9%. A wide disease spectrum was implicated. This patient group has a high admission rate (47.8%) and a high mortality rate (31.3%). The deaths occurred largely in the elderly and it is suggested that elderly patients should either be admitted for observation, or a careful screening carried out for underlying pathology. The diversity of disease precludes a standard management protocol.

Adolescent↗
PubMed1993

cis-1,2,3a,4,5,9b-hexahydro-3H-benz[e]indoles: synthesis and in vitro binding affinity at dopamine D1 and D2 receptors.

cis-1,2,3a,4,5,9b-Hexahydro-3H-benz[e]indoles were synthesized and evaluated for in vitro dopamine D1 and D2 receptor binding affinity. The target compounds 21-25 were readily prepared by reduction of the air-sensitive tricyclic enamines 10-14. Reduction of 10-14 with sodium borohydride, sodium cyanoborohydride, palladium on carbon in ethanol, and platinum oxide in ethanol or acetic acid gave only the cis (3a,9b) 1,2,3a,4,5,9b-hexahydro-3H-benz[e]indoles. The stereochemistry was confirmed by single-crystal X-ray analysis. In the 6-hydroxy series, the binding affinity at D1 and D2 receptors was of the order 22 (N-n-butyl) > 21 (N-n-propyl) > 23 (N-H). The compounds demonstrated greater binding affinity at D2 receptors than at D1 binding sites. In contrast, 8-OH derivatives exhibited affinity only for D2 receptors, with 25 (N-n-butyl) having slightly greater affinity than 24 (N-n-propyl).

Animals↗
PubMed1993

An interpretation of transference.

This paper offers an interpretation of the concept of transference. It begins with a re-examination of Socrates's therapeutic intent and Plato's revisions of psychological theory in the light of Socrates's failure. In particular, Plato devised an account of a structured psyche, a theory of fantasy, and a complex 'object-relations' theory, to explain dynamic interactions between psyche and social world. It is argued that these revisions embody a recognition of the phenomenon of transference, i.e. the psyche's characteristic activity of creating a meaningful world in which to live. Freud's early conception of transference--as a transfer of psychological content across space and time--is criticised on the ground that it assumes that the world is already given, independent of any psychic activity. Freud's later conception of transference as a repetition is then explored in the light of the psyche's ability to create artefacts. It is argued that neurotic transference is the unconscious attempt to create an idosyncratic polis, an idiopolis, in which to live. The resolution of the transference occurs because the analyst is made a citizen of the idiopolis, has learned the idiolect, and can speak in that idiolect of the fundamental conflicts within the idiopolis and their dynamic basis. A neurotic world cannot survive this internal recognition.

Freudian Theory↗
PubMed1990

Pharmacokinetics, biodistribution, and gamma camera imaging of 111In-KC-4G3 murine monoclonal antibody in athymic nude mice with or without human tumor xenografts.

The pharmacokinetics and tissue distribution of the monoclonal antibody radioconjugate 111In-diethylenetriaminepentaacetic acid-KC-4G3, which is directed against a high molecular weight mucin(s) antigen expressed on the human milk fat globule and many epithelial cell membranes, were examined in BALB/c nude mice with and without xenografts of the human tumor lines ZR-75 (mammary adenocarcinoma, KC-4G3 antigen positive) and BALL-1 (B-cell lymphoma, KC-4G3 antigen negative). Plasma of ZR-75 and BALL-1 tumor-bearing nude mice inoculated with 111In-KC-4G3 had a higher initial volume of distribution (V1), steady state volume of distribution (Vss), and plasma clearance and a lower initial half-life (t1/2 alpha) than non-tumor-bearing nude mice. There were no significant differences in biological half-life (t1/2 beta) in tumor- and non-tumor-bearing nude mice. Urinary and fecal excretion of radioactivity by ZR-75 tumor-bearing mice was greater than that of BALL-1 and non-tumor-bearing mice. Localization of 111In-KC-4G3 in mice bearing xenografts of ZR-75 was significantly greater than in mice with BALL-1 tumors. Uptake of 111In-KC-4G3 by ZR-75 tumors averaged 14% of injected dose/g at 72 h after inoculation and was unaffected by antibody dose. Significantly, the radioconjugate concentration in ZR-75 tumors remained relatively constant from 72 to 336 h post-inoculation, while that in normal tissues declined considerably over this period. Nonspecific reticuloendothelial tissue uptake of 111In-KC-4G3 was only moderately affected by pretreatment with a large excess of unlabeled normal mouse immunoglobulin and was not changed by treatment with asialofetuin. Further enhancement of specific localization of 111In-KC-4G3 was obtained by subtraction of the blood pool identified by co-inoculation of 131I-labeled, isotype-identical, normal mouse immunoglobulin. Gamma camera images of 111In-KC-4G3-inoculated ZR-75 tumor-bearing mice showed enhanced tumor localization compared to mice with BALL-1 tumors. The results of this study suggest that 111In-KC-4G3 may prove useful for imaging and possibly therapy of human malignancies expressing the high molecular weight epithelial mucin(s).

Animals↗
PubMed1983

Neuronal response of the hippocampal formation to injury: blood flow, glucose metabolism, and protein synthesis.

The reaction of the hippocampal formation to entorhinal lesions was studied from the viewpoints of cerebral blood flow ([123I]isopropyl-iodoamphetamine[IMP])-glucose utilization ([14C]2-deoxyglucose), and protein synthesis ([14C]leucine), using single- and double-label autoradiography. Our study showed (i) decreased glucose utilization in the inner part, and increased glucose utilization in the outer part of the molecular layer of the dentate gyrus, starting 3 days after the lesion; (ii) increased uptake of [123I]IMP around the lesion from 1 to 3 days postlesion; and (iii) starting 3 days after the lesion, marked decrease in [14C]leucine incorporation into proteins and cell loss in the dorsal CA1 and dorsal subiculum in about one-half of the rats. These changes were present only in animals with lesions which invaded the ventral hippocampal formation in which axons of CA1 cells travel. By contrast, transsection of the 3rd and 4th cranial nerves resulted, 3 to 9 days after injury, in a striking increase in protein synthesis in the oculomotor and trochlear nuclei. These results raise the possibility that in some neurons the failure of central regeneration may result from the cell's inability to increase its rate of protein synthesis in response to axonal injury.

Amino Acids↗