Folkers, Karl Bowers, Cyril Y. Stepinski, Janusz Plucinski, Tomasz Sakagami, Masanori Kubiak, Teresa
Published in
Zeitschrift für Naturforschung B
Twenty-four new analogs of the luteinizing hormone releasing hormone (LHRH) were synthesized and bioassayed for antiovulatory activity in rats. [N-Ac-3⊿Pro1, pF-D-Phe2, D-Trp3,6, Azagly10]-LHRH com pletely inhibited ovulation at 6 μg and was the most potent of the 24, and is a relatively potent antagonist in the field. The Azagly- and Ac-NHNH- and ...
Peterson, T C
Published in
The Canadian journal of infectious diseases = Journal canadien des maladies infectieuses
Cytokine antagonists are a group of drugs defined by their actions on specific cytokines. Cytokine antagonists can inhibit action of cytokines by acting directly on receptors, by affecting production of cytokines or by binding to cytokines and preventing their subsequent action. Recent evidence suggests that Hansen's disease, which is characterized...
Parsons, C. G. Danysz, W. Hesselink, M. Hartmann, S. Lorenz, B. Wollenburg, C. Quack, G.
Published in
Amino Acids
Glycine is a co-agonist at NMDA receptors and it's presence is a prerequisite for channel activation by glutamate or NMDA. Physiological concentrations reduce one form of NMDA receptor-desensitization. Interactions between the glycineB site and other domains of the NMDA receptor are complex and include the glutamate, Mg+ and polyamines sites. Glyci...
Huang, Li-Hua Li, Jian-Li Wang, Shu-Rong
Published in
Brain, Behavior and Evolution
Neuronal responses of 114 cells to electrical stimulation of the optic tectum were extracellularly recorded from the contralateral nucleus rotundus (nRt) in pigeons (Columba livia), and the effects of two glutamatergic antagonists CNQX and CPP, as well as those of GABA, were examined on rotundal cells. The results show that tectal stimulation evoke...
Francis-West, P. H. Parish, Joanne Lee, Kevin Archer, Charles W.
Published in
Cell and Tissue Research
The synovial joint arises from an initial condensation of cells that subsequently develops into distinct skeletal structures, separated by the joint. Bone morphogenetic proteins (BMPs) and growth and differentiation factors (GDFs) have a fundamental role during skeletogenesis, including joint formation. Development of the joint appears to be depend...
Tarzia, Giorgio Diamantini, Giuseppe Spadoni, Gilberto
Published in
Neurosignals
This article reviews our efforts in the development of indole melatonin (MLT) agonist and antagonist compounds. Evidence is presented which indicates that high-affinity melatonergic agonists were obtained by shifting the MLT amido side chain from the C-3 to the N-1 indole position. Conversely, by moving the side chain from the C-3 to the C-2 indole...
Iwasa, Satoshi Fan, Jianglin Miyauchi, Takashi Watanabe, Teruo
Published in
Pathobiology
Objective: Endothelin (ET)-1 has proatherogenic properties, since ET receptor antagonists reduce atherosclerotic lesions in animals. However, we recently demonstrated that ET-1 and ETB receptors are increased in atherosclerotic lesions. To further examine the effects of ETB receptor antagonism on atherogenesis, we investigated the chronic effects o...
Tohei, Atsushi Matsuzaki, Minako Kogo, Hiroshi
Published in
Neuroendocrinology
Pituitary adenylate cyclase activating polypeptide (PACAP) is a relatively new neuropeptide, and it has a potent stimulatory effect on adenylate cyclase activity in rat pituitary cells. However, the role of PACAP in the physiological control of prolactin (PRL) secretion is still unclear. In the present study, we investigated the physiological signi...
Thibonnier, M. Coles, P. Thibonnier, A. Shoham, M.
Published in
Progress in Brain Research
AVP receptors represent a logical target for drug development. As a new class of therapeutic agents, orally active AVP analogs could be used to treat several human pathophysiological conditions including neurogenic diabetes insipidus, the syndrome of inappropriate secretion of AVP (SIADH), congestive heart failure, arterial hypertension, liver cirr...
Van Bever, H.P.S.
Singapore Paediatric Journal / 44 / 2 / 42-47 / SPJOF
