1,25-Dihydroxyvitamin D3 [1,25-(OH)2D3] receptor concentration was measured by an accurate immunoradiometric assay in primary tumors from 10 patients with colorectal carcinoma and 11 patients with non-small cell carcinoma of the lung. Measurements were also performed on a noncancerous sample of the same origin as the tumor from each patient. All of the tumors contained receptor with a mean conc...

Background Opiate addiction is associated with complex cognitive impairment, which contributes to the development of compulsive drug use and relapses. Dopamine and N-methyl-D-aspartate receptors play critical roles in opiate-induced cognitive deficits. However, the roles of D1 and D3 receptors in the N-methyl-D-aspartate/glycineB receptor-regulated cognitive behaviors induced by morphine remain...

Previously, we developed a proteolytically stable small molecule peptidomimetic termed D3 as a selective ligand of the extracellular domain of the TrkA receptor for the NGF. Ex vivo D3 was defined as a selective, partial TrkA agonist. Here, the in vivo efficacy of D3 as a potential therapeutic for cholinergic neurons was tested in cognitively impaired aged rats, and we compared the consequence ...

The mesolimbic dopaminergic system plays a primary role in mediating the euphoric and rewarding effects of most abused drugs. Chronic cocaine use is associated with an increase in dopamine neurotransmission resulting from the blockade of dopamine uptake and is mediated by the activation of dopamine receptors. Recent studies have suggested that the D3 receptor subtype plays a pivotal role in the...

The relationship between activation-induced growth inhibition and regulation of the cell cycle progression was investigated in T cell hybridomas by studying the function of the cell cycle-regulating genes such as G1 cyclins and their associated kinases. Activation of T cell hybridomas by anti-T cell receptor antibody induces growth arrest at G1 phase of the cell cycle and subsequently results i...

Metabolism of [3H]25-hydroxyvitamin D3(25-OH-D3) was studied in primary cultures of pulmonary alveolar macrophages (PAM) from seven patients with sarcoidosis and two patients with idiopathic pulmonary fibrosis. Production of a [3H]1,25-dihydroxyvitamin D3 (1,25-[OH]2-D3)-like metabolite of [3H]25-OH-D3 was detected in lipid extracts of cells from five patients with sarcoidosis. Synthesis of thi...

The dopamine 3 (D3) receptor is a promising therapeutic target for the treatment of nervous system disorders, such as Parkinson's disease, and current research interests primarily focus on the discovery/design of potent D3 agonists. Herein, a well-designed computational protocol, which combines pharmacophore identification, homology modeling, molecular docking, and molecular dynamics (MD) simul...

The 1,25-dihydroxyvitamin D3 receptor from porcine intestine has been characterized by immunoprecipitation and immunoblotting experiments. Immunoprecipitation studies demonstrate that monoclonal antibodies to the receptor that recognize two different epitopes on the receptor protein quantitatively precipitate the 1,25-dihydroxyvitamin D3 binding activity from nuclear and whole cell extracts of ...

AIMS To determine whether the vitamin D receptor is expressed in colorectal cancer, and its relation to stage of disease. METHODS Paraffin embedded sections of colorectal cancer from 30 patients who had undergone surgery were studied. Immunohistochemistry using the specific monoclonal antibody 9A7 gamma directed against the nuclear vitamin D receptor was used to identify receptors for the act...

Dopamine (DA) autoreceptors expressed along the somatodendritic extent of midbrain DA neurons modulate impulse activity, whereas those expressed at DA nerve terminals regulate both DA synthesis and release. Considerable evidence has indicated that these DA autoreceptors are of the D2 subtype of DA receptors. However, many pharmacological studies have suggested an autoreceptor role for the DA D3...