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W Utz

Publications and source records attributed to W Utz.

At least 19 recordsLinked to original sources
PubMed2001

Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).

Structure dependent efficacy studies in the field of selective D4 ligands led to the 2-aminomethyl substituted azaindole 2 (FAUC 213) that displayed strong D4 binding, high subtype selectivity, and complete antagonist properties in ligand-induced mitogenesis experiments. According to our schematic molecular model, the intrinsic activity of the regioisomers investigated is controlled by the ability of the heterocyclic unit to interact with both elements of the D4 binding-site crevice, the aromatic microdomain in TM6, and a serine residue in TM5.

Animals↗
PubMed2001

Comparative molecular field analysis of dopamine D4 receptor antagonists including 3-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 113), 3-[4-(4-chlorophenyl)piperazin-1-ylmethyl]-1H-pyrrolo-[2,3-b]pyridine (L-745,870), and clozapine.

A CoMFA study was undertaken to elucidate the correlation of biological activity and structural parameters of 25 dopamine D4 antagonists. A special point of interest is that we have included the atypical D4 antagonist clozapine as a structural template for all other compounds. After comparing potential protonation sites at semiempirical (AM1) and ab initio (6-31G(d)) levels of theory, possible conformations of the lead compound 3-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 113) were investigated by systematic semiempirical conformational analysis. The final conformation of FAUC 113, which was used as a template for the other compounds in the dataset, was chosen by clustering and rigid body alignment of all conformations to clozapine. The CoMFA applied on the final alignment resulted in a q2cv of 0.739. To elucidate the influence of the absolute orientation of the molecules within the grid space, the entire dataset was systematically rotated (1296 steps) within the lattice. The Gaussian-shaped distribution of the q2cv values spanned the range of 0.699-0.794 and therefore supports the significance of the analysis.

Clozapine↗
PubMed2000

Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonists recognizing preferentially the D(3) subtype.

To evaluate nonaromatic catechol bioisosteres, the conformationally restrained enynes 1 and enediynes 2 were synthesized via palladium-catalyzed coupling as the key reaction step. Subsequent receptor binding studies at the dopamine receptor subtypes D(1), D(2 long), D(2 short), D(3), and D(4) showed highly interesting binding profiles for the enynes 1a and 1b when compared to dopamine. At the guanine nucleotide-sensitive high-affinity binding site of the D(3) receptor, the target compound 1b (K(i) = 5.2 nM) was 10-fold more potent than dopamine but less potent at the D(2) and D(4) subtypes. In contrast to dopamine the agonists 1a and 1b showed strong selectivity for the receptors of the D(2) family (D(2)-D(4)). As far as we know, this study represents the first report on nonaromatic dopamine agonists. Comparison of molecular electrostatic potentials, derived from semiempirical molecular orbital calculations, and lipophilicity maps was performed.

Alkynes↗
PubMed1984

Multifocal dermal-type basal cell adenomas of parotid glands with co-existing dermal cylindromas.

A basal cell adenoma of the parotid gland accompanied by multiple developing microadenomas of the same type and three dermal cylindromas, all observed in a 54-year-old woman, were examined by light microscopy. The histological structure of the basal cell adenomas shows striking similarities to co-existing dermal cylindromas, suggesting a common histogenesis of both tumors. We suggest that the term "basal cell adenoma of dermal type" should be used for these lesions. Multifocal ductal proliferations with nascent adenomas in the glandular parenchyma allow us to trace the development of these tumors. Studies of the literature reveal four additional cases in which there are co-existing basal cell adenomas of salivary glands and dermal adnexal tumors.

Adenoma↗
PubMed1977

[Bone regeneration over plastic implants after mandibular resection breaking the continuity].

In young patients, bone regeneration may start from the region of the temporo-mandibular joint and from the peripheral mandibular stump in cases of continuity defects of the mandible. A resin graft implanted for soft tissue reconstruction is collar-like surrounded by bone which is developing into a functionally and anatomically full regenerate over many years, in correspondence to periosteal and desmal growth stimuli. In adults, regeneration is minimal.

Adolescent↗
PubMed1977

[Clinical aspects of osteomyelitis sicca (pseudo-Paget)].

Osteomyelitis sicca of the mandible in its dry, tumour-producing form was described clinically and radiologically as pseudo-Paget's disease by Axhausen in 1934. In 1969, Hoppe et al. were able to corroborate in animal experiments different stages of this disease, previously outlined by Hoppe in a pathological histological study in 1964. Empirically, an anti-rheumatic treatment offers itself with which an exacerbation can be cut short and complete remission obtained later.

Adolescent↗
PubMed1976

[Results of conservative and surgical treatment of jaw fractures].

In the majority of the patients with fractures of the jaws treated in the period covered by this study, conservative therapy has shown satisfying results. In intraoral splinting, periodontal lesions could largely be avoided by adequate oral hygiene. Surgery must still be applied in those cases where conservative methods failed to be successful.

Fracture Fixation↗
PubMed1976

[Clinical aspects and pathology of tumors of the temporomandibular joint].

Two primary tumors of the temporo-mandibular joint are presented. Because of their unspecific clinical symptoms, the diagnosis could be confirmed by surgical intervention and histopathology only after a long period of observation. Benign temporo-mandibular joint tumors can still be managed, while in malignant tumors the further course of the disease is characterized by a poor prognosis.

Adult↗
PubMed1976

[Transsinusal repositioning and retention of zygomatic fractures].

In the treatment of impression fractures of the zygoma transsinusal repositioning of the fragments and their retention by means of a simple inflatable balloon catheter has proved successful. This method not only permits retention and drainage of the maxillary sinus but also postoperative correction of visual disturbances, if necessary.

Adolescent↗