Hormones analogues

Structure—Activity Relationships. In spite of the considerable synthetic and bioassay effort involved in estabhshing the thyromimetic potency of thyroid-hormone analogues, more than 100 compounds have been studied (Table 2). The main stmctural requirements for thyromimetic activity can be summarized as follows (6,12—16). 

A large number of thyroid hormone analogues have been tested for this effect (6). Among others, i-T (3) and 3,3 -T2 (5) and their propionic acid side-chain analogues decrease oxygen consumption at molar ratios of 50—200 1 of T. Nevertheless, no potent or clinically usehil peripheral antagonists have been found. 

Jaffe, H., Hayes, D. K., Lutra, R. P., Shuka, P. G., Amarnath, N., and Chaney, N. A., Controlled release micro-spheres of insect hormone analogues, Proc. Int. Symp. Control. Rel. Bioact. Mater., 12, 282, 1985. 

Leucoquinizarin, 9 328-329 Leucoxenes, 25 31, 33 Leukocytes, 4 83, 89 Leuprolide acetate formulations, encapsulated, 76 453 Leurocristine (vincristine), 2 77, 98, 99 Leuseramycin, 20 136 Leutinizing hormone releasing hormone analogue, registered for use in aquaculture in Australia, 3 222t Levans, 23 481 in beets, 23 463... 

Hoitink, M. A., Hop, E., Beijnen, J. H., Bull, A., Kettenes-van den Bosch, J. J., and Underberg, W. J. M. (1997). Capillary zone electrophoresis mass spectrometry as a tool in the stability research of the luteinising hormone-releasing hormone analogue goserelin.. Chromatogr. A 776, 319—327. 

Within a programme aimed at the development of thyroid hormone analogues as potentially useful plasma cholesterol-lowering agents, the pyrida-zinone derivative SK F L-94901 (98) has been prepared and investigated in the U.K. [419-422]. Whereas naturally occurring thyroid hormones cannot be employed for this purpose because of their undesirable effect on heart rate, (98) has been found to represent a potent thyromimetic which retains hepatic activity but lacks cardiac activity. Structural modifications and QSAR studies have been carried out [422]. 

Drug Action - The action of a drug or poison refers to its biochemical mechanism. How does it interact on a molecular level A drug may interferewith membrane permeability, for example. Or it may be an enzyme inhibitor, hormone analogue and competitor, or DNA intercalator. Let us consider some specific drug actions. 

Homogeraniol is an important intermediate in syntheses of squalene, aplyslstatin,8 dendrolasin,9 and juvenile hormone analogues.18 The present procedure affords an efficient, stereoselective method for preparing (E)-homogeraniol, contaminated by at most 1-2% of the Z isomer. 

Amino N, Hidaka Y, Takano T, Tatsumi K, Izumi Y, Nakata Y. Possible induction of Graves disease and painless thyroiditis by gonadotrophin-releasing hormone analogues. Thyroid 2003 8 815-8. 

Toussirot E, Wendling D. Fibromyalgia developed after administration of gonadotrophin-releasing hormone analogue. Clin Rheumatol 2001 20(2) 150-2. 

Paoletti AM, Serra GG, Cagnacci A, Vacca AM, Guerriero S, Solla E, Melis GB. Spontaneous reversibility of bone loss induced by gonadotropin-releasing hormone analogue treatment. Fertil Steril 1996 65(4) 707-10. 

Pierce SJ, Gazvani MR, Farquharson RG. Long-term use of gonadotropin-releasing hormone analogues and hormone replacement therapy in the management of endometriosis a randomized trial with a 6-year follow-up. Fertil Steril 2000 74(5) 964-8. 

Because its vasoconstrictor effects limit the use of the native hormone, analogues with greater or lesser affinity for vasopressin V2 receptors and more selective antidiuretic effects have been developed ... 

Okada, H., et al. 1983. Vaginal absorption of a potent luteinizing hormone-releasing hormone analogue (leuprolide) in rats. IV. Evaluation of vaginal absorption and gonadotropin responses by radioimmunoassay. J Pharm Sci 73 289. 

Chiellini, G. Nguyen, N.-H. Apriletti, J. W. Baxter, J. D. Scanlan, T. S. Synthesis and biological activity of novel thyroid hormone analogues 5 -aryl substituted GC-1 derivatives. Bioorg. Med. Chem. 2002, 10, 333—346. 

Mousa SA, O Connor LJ, Bergh JJ, et al, The proangiogenic action of thyroid hormone analogue GC-I is initiated at an integrin, J Cardiovasc Pharmacol 2005 46 356-360,... 

Endocrine drugs Antiandrogens, oestrogens, gonadotropinreleasing hormone analogues ... 

Rondot I., Quennedey B., Courrent A., Lemoine A. and Delachambre J. (1996) Cloning and sequencing of a cDNA encoding a larval-pupal-specific cuticular protein in Tenebrio molitor (Insecta, Coleoptera). Developmental expression and effect of a juvenile hormone analogue. Eur. J. Biochem. 235, 138-143. 

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