Hormonally Active Brain Peptides : Structure and Function

Near the end of September 1980, the contributors to Hormonally Active Brain Pep tides: Structure and Function met to discuss their chapters for the monograph. This meeting was the eighth sponsored by the International Foundation for Biochemical Endocrinology and was held at the Hotel Plakir in Dubrovnik, Yugoslavia. Several months were allowed after the meeting for the contributors to revise their manuscripts and for editing. Professor Dr. Vladimir Pantie and the Serbian Academy of Sciences and Arts were in charge of the local arrangements and social activities. The Foundation is grateful for the splendid job that was done and for the out­ standing scientific, cultural, and social activities. I thank the Serbian Acad­ emy of Sciences and Arts and the Yugoslav Council of Academies for spon­ soring my stay in Yugoslavia. I greatly enjoyed giving lectures, visiting laboratories, and discussing research projects in a number of centers in Yugoslavia. A diverse group of topics was presented in Dubrovnik concerning cer­ tain brain peptides. The topics included "Structure, Function, and Confor­ mation of Neuropeptides," "Distribution of Peptides in the Brain," "Reg­ ulation of the Release of Peptide Hormones," "The Active Center of Gonadotropins," "In Vitro Synthesis of Hypothalamic Hormones," "Stud­ ies on Gonadotropin-Releasing Hormone," "Studies on the Biosynthesis, Release, and Degradation of LH-RH," "Genesis and Properties of Pitu­ itary ACTH, Prolactin, and Growth Hormone Producing Cells," "Precur­ sors to Oligopeptide Hormones," and "Stress Effects on Peptide Hormone Synthesis.

1 Structure and Function Relationships among Synthetic Enkephalin Analogues.- 1. Introduction.- 2. Opiate Activity of Enkephalins and ?-Endorphin.- 3. Design and Synthesis of Enkephalin Analogues with Improved Opioid Activity.- 4. Modification at the N Terminus.- 5. Modification at the C Terminus.- 6. Conclusions.- Discussion.- References.- 2 Secondary Structure — Function Relationships in ?-Endorphin: A Proposed Model of the Biologically Active Conformation.- 1. Introduction.- 2. Circular Dichroism Studies.- 3. Predictive Analysis of the Secondary Structure.- 4. Correlation between the Solution Conformation and Biological Activity.- References.- 3 Studies on the Conformation of Neuropeptides.- 1. Introduction.- 2. Material and Methods.- 3. ACTH.- 4. Angiotensin II.- 5. Thyroliberin.- 6. Conclusion.- Discussion.- References.- 4 The Search for the Active Center of the Gonadotropins.- 1. Introduction.- 2. Methods in Peptide Synthesis.- 3. Testing of Inhibitory Peptides.- 4. Discussion.- 5. Summary.- 6. Projections for the Future.- Discussion.- References.- 5 Hormonal Antagonistic Properties of Deglycosylated Pituitary Lutropin.- 1. Introduction.- 2. Preparation of Deglycosylated LH.- 3. Biological Properties of DG-LH.- 4. Concluding Comments.- References.- 6 Hormonal Regulation of and Ionic Requirements for in Vitro Release of Hypothalamic Peptides.- 1. Introduction.- 2. Effects of Neurotransmitters or Neuropeptides on Hypothalamic Hormone Release in Vitro.- 3. Interaction of Opiates with LH-RH and SRIF Release.- 4. Ionic Requirements of Neuropeptide Release.- 5. Are Neuropeptide-Neurotransmitter Interactions Coupled with Ionic Channels?.- 6. Hormonal Effect on Neuropeptide Release in Vitro.- 7. Conclusion.- References.- 7 In Vitro Release of Luteinizing Hormone-Releasing Hormone: Influence of Estrogen and a Mammary Carcinogen.- 1. Introduction.- 2. Methods.- 3. Results.- 4. Discussion.- Discussion.- References.- 8 Mode of Opioid and Catecholamine Involvement in Regulating LH Secretion.- 1. Introduction.- 2. Effects of Opiates on LH Release.- 3. Effects of Opiate Receptor Antagonists on Pituitary LH Release.- 4. Effects of Estrogen on LH Release Induced by Naloxone.- 5. Mode of Opiate Involvement in Pituitary LH Release.- 6. Site(s) of Opiate Modulation of LH Release.- 7. Summary.- Discussion.- References.- 9 Stress, Corticoliberin (CRF), and Glucocorticoids in the Regulations of ACTH Release.- 1. Introduction.- 2. ACTH-Secreting Cells.- 3. The Nature of CRF.- 4. The Site of CRF Release.- 5. The Location of CRF-Producing Cells.- 6. Afferent Pathways of Stressful Stimuli.- 7. Feedback Regulation of ACTH Secretion.- References.- 10 The Role of Steroid Receptors in the Regulation and Integration of Steroid and Peptide Hormone Actions in Common Target Cells: Facts and Speculations.- 1. Introduction.- 2. The Basic (Hypothetical) Concepts of the Proposed Model for Integrating the Actions of Steroid and Peptide Hormones in Common Target Cells.- 3. Experimental Facts Supporting the Basic Concepts of the Proposed Model.- 4. Coordination and Integration of Steroid and Peptide Hormone Actions in Common Tar get Cells.- 5. Potentiation.- 6. The Model—Description, Postulates, and Speculations.- 7. Summary and Prospects for the Future.- Discussion.- References.- 11 Effects of Estrogens on Receptor “Nucleotropy” and “Activation”.- 1. Introduction.- 2. Subcellular Origins and Properties of Uterine Estradiol Receptors.- 3. Reactions of Uterine Cells to Pulse-Administered Estradiol.- 4. Receptor “Nucleotropy” and “Activation”.- 5. Ovarian- and Steroid-Independent Fluctuations of Uterine Estradiol Receptor Action.- 6. The Basic Mechanism of Estradiol Receptor Action.- 7. How to Succeed in Mapping the Steroid-Sensitive Areas of the Brain.- References.- 12 Steroids and Membrane-Associated Events in Neurons and Pituitary Cells.- 1. Introduction.- 2. The Electrophysiological Approach.- 3. Electrophysiological Approach to the Study of Sex Steroid Effects on Neurons.- 4. Electrophysiological Approach to the Study of Sex Steroid Effects on Pituitary Cells.- 5. Concluding Remarks.- Discussion.- References.- 13 Electrical Effects of Steroids in Neurons.- 1. Introduction.- 2. Effects of Estrogen on Hypothalamic Neurons.- 3. Effects of Other Steroids (Progesterone, Testosterone, and Cortisol) on Hypothalamic Neurons.- 4. Effects of Steroids on Behavior-Related Electrophysiological Events.- 5. Conclusion and Prospectus.- References.- 14 Recent Data on Neuropeptide Mapping in the Central Nervous System.- 1. Introduction.- 2. Distribution of Neuropeptides in the Major Brain Areas.- 3. Peptidergic Axons in Major Anatomical Pathways.- 4. Concluding Remarks.- References.- 15 Distribution and Changes in Peptides in the Brain.- 1. Introduction.- 2. Distribution of Neurotransmitter Peptides in Brain.- 3. Physiological Changes in Opiate Peptide Distribution.- 4. Effects of Hypothyroidism on Brain Peptides.- References.- 16 In Vitro Synthesis of Hypothalamic Neurophysin Precursors.- 1. Introduction.- 2. Cell-Free Synthesis and Immunological Recognition of Neurophysic-Related Translation Products.- 3. Chemical Verification that Neurophysin-Related Translation Products Contain Neurophysin Amino Acid Sequences.- 4. Identity of Translation Products as Biosynthetic Precursors.- 5. Nucleic Acid-Precursor Interrelationships.- 6. Relationship between Neurophysin and Neuropeptide Hormone Biosynthesis.- 7. Future Directions—the Chemical Basis of Neurophysic-Neuropeptide Folding and Function.- References.- 17 Steroid Antagonism of Melanosome Movements Induced by Neuropeptides.- 1. Effects of ACTH and Related Peptides and of Glucocorticoids on the Brain.- 2. The Amphibian Melanophore as a Model.- 3. Effects of Corticosteroids on Frog Skin Melanophores.- 4. Summary 362 References.- 18 Is VIP a Neuroregulator or a Hormone?.- 1. Introduction.- 2. Source of VIP.- 3. VIP as a Regulatory Peptide.- 4. Biological Effects and Receptors of VIP.- 5. Conclusion: VIP as Neuroregulator.- Discussion.- References.- 19 Gonadotropin-Releasing Hormone: Release into Hypophyseal Portal Blood and Mechanism of Action.- 1. Introduction.- 2. Gonadotropin Release into Hypophyseal Portal Blood Evoked by Electrical Stimulation.- 3. Spontaneous Release of GnRH into Hypophyseal Portal Vessel Blood.- 4. Changes in Pituitary Responsiveness to GnRH.- 5. The Neural Mechanism Responsible for Diurnal and Episodic Release of LH.- 6. Mechanism of Action of GnRH.- 7. Summary.- References.- 20 Biodegradation of Luteinizing Hormone-Releasing Hormone.- 1. Introduction.- 2. Disappearance of LH-RH in Vivo.- 3. Biodegradation of LH-RH in the CNS and Pituitary.- 4. Physiological Significance of LH-RH Biodegradation.- Discussion.- References.- 21 Ultrastructural Characteristics of Proteinergic Synthesis in the Pineal Gland.- 1. Introduction.- 2. Materials and Methods.- 3. Results.- 4. Discussion.- Discussion.- References.- 22 Peptidergic Activity of the Pineal Gland in Stress.- 1. Introduction.- 2. Aim of Investigation.- 3. Materials and Methods.- 4. Results.- 5. Discussion.- Discussion.- References.- 23 Effect of Colchicine on the Stress-Type ACTH Release in Rats.- 1. Introduction.- 2. Experimental Approaches.- 3. Results and Discussion.- 4. Conclusion.- References.- 24 Genesis and Properties of Pituitary ACTH, MSH, Prolactin, and GH Producing Cells.- 1. Introduction.- 2. The Aim of This Article.- 3. Origin and Nature of ACTH and MSH.- 4. Pars Intermedia.- 5. Common and Specific Properties of PRL and GH Cells.- 6. Regulation of PRL and GH Release and Synthesis.- 7. The Role of Gonadal Steroids in PRL Cell Genesis and Hormone Release.- 8. Concluding Remarks.- References.- 25 Interaction between Thyrotropin-Releasing Hormone and Prolactin-Producing Cells.- 1. Introduction.- 2. Binding of [3H]-TRH to GH3 Cells.- 3. Adenosine 3?,5?-Cyclic Nucleotide Phosphodiesterase(s) in GH3 Cells.- 4. Studies on the Role of Calcium in the Control of PRL Secretion.- 5. Conclusions.- References.- 26 Cell-Free Synthesis of Rat Lutropin Subunits.- 1. Introduction.- 2. Cell-Free Synthesis of LH Subunits.- 3. Conclusions and Projections.- 4. Summary.- References.- 27 Cellular Polyproteins from Pituitary and Hypothalamus: Composite Precursors to Oligopeptide Hormones.- 1. Introduction.- 2. Definition and Significance of Cellular Polyproteins.- 3. General Comments on the Synthesis and Identification of Precursors to Oligopeptide Hormones.- 4. The Pituitary Polyprotein Prepro-opiocortin.- 5. Hypothalamic Polyproteins.- 6. The Search for Precursors to Somatostatin and LH-RH.- References.- 28 Tritium Labeling of Brain Peptides.- 1. Introduction.- 2. Methods for Tritium Labeling of Peptides.- 3. Tritium Labeling of Brain Peptides.- 4. Conclusion.- References.- Appendix Members of the International Foundation for Biochemical Endocrinology.