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CONTENTS
DiePharmazie Supplement 07/1997

Session 1

Bodor, N.: Retrometabolic drug design concepts S 5

Bialer, M.: The utilization of structure pharmacokinetic pharmacodynamic relationship (SPPR) approach to develop GABA and glycine derivatives as new and better antiepileptics
S 5

Kitazawa, E.; Iwabuchi, H.; Kogen, H.; Tsujita, Y.: Study on the improvement of pravastatin sodium via the quantitative structure-metabolism relationship S 6

Ebert, B.; Frlund, B.; Falch, E.; Krogsgaard-Larsen, P.: Design of specific GABA-A receptor agonist drugs considering efficacy and pharmacokinetic and metabolism parameters S 6

Fujii, I.: Prodrug activation via catalytic antibodies S 7


Session 2


Amidon, G. L.: Peptide transporter based prodrug design: opportunities for improving the permeability of a polar drug S 8

Hussain, A. A.: A rational approach to the administration of L-DOPA prodrugs nasally for the treatment of parkinson's disease S 8

Murakami, T.; Nishimura, K. Mori, N.; Yata, N.: Bifunctional prodrugs for the improvement of oral bioavailability S 9

Suarez, S.; Gonzales-Rothi, R.; Hochhaus, G.: The effect of dose and release rate on pulmonary targeting of glucocorticoids using liposomes as a model dosage form S 9

Watanabe, S.; Kawai, H.; Fukui, M.: Novel colon-specific delivery system: improvement of oral peptide absorption S 10


Session 3

Nagai, T.; Shimizu, K.; Maitani, Y.; Talayama, K.: Liver targeting liposomes containing soybean-derived sterolglycosides S 11

Brewster, M.; Pop, E.; Bodor, N.: Brain-enhanced delivery of zidovudine through the use of redox targeting S 11

Hata, T.; Fujisaki, J.; Hirabayashi, H.; Kimura, S.: Targeting of drug: osteoporotic drug delivery system via pro-drug S 12

Simpkins, J. W.; Rajakumar, G.; Rabbani, O.; Panickar, K.; Simpkins, C. E.; Day, A. L.; Bodor, N.: Traetment of Alzheimer's disease and stroke through the preferential delivery of estrogens to the brain S 12

Visser, P.; Brummelhuis, M.; Chikhale, P.: Bioreductively-activated carriers for targeting anticancer agents to solid tumors S 13

Prokai, L.; Prokai-Tetrai, K.; Xudong Ouyang, Whei-Mai Wu; Jiaxiang Wu, Ho-Seung Kim; Zharikova, A.; Simpkins. J.; Bodor, N.: Retrometabolic drug design for brain targeting of thyrotropin-releasing hormone analogs S 13


Session 4


Houghten, R. A.: Combinatorial library strategies for the identification of highly active compounds S 14

Pop, E.; Brewster, M.: Optimization of the properties of brain specific chemical delivery systems by structural modifications
S 14

Darvas, F.: Computer-assisted evaluation of a combinatorial library for retrometabolic drug optimization S 15

Takayama, K.; Takahara, J.; Nagai, T.: Formula optimization based on artificial neural networks in ketoprofen dermal gels containing o-ethylmenthol S 15

Bodor, N.; Buchwald, P.: Molecular size based approach to estimate partition properties S 16


Session 5


Sugiyama, Y.; Suzuki, H.; Kato, Y.: Pharmacokinetic approach for drug targeting: use of carrier-mediated and receptor-mediated transport mechanism S 17

Derendorf, H.; Hochhaus, G.; Meibohm, B.; Möllmann, H.; Barth, J.: Pharmacokinetics and pharmacodynamics of soft corticosteroids for inhalation S 17

Otagiri, M.; Imai, T.; Fukuhara, A.: Pharmacokinetic studies on the reduction of flurbiprofen-induced gastric damage trough chimeria drug formation S 18

Hakusui, H.; Atsumi, R.: Retrometabolism of irinotecan(CPT-11), a promising water-soluble analogue of camptothecin S 18

Imai, T.; Yoshigae, Y.; Otagiri, M.: First-pass metabolism of propranolol prodrug S 19

Druzgala, P.; Dennis, D.: Soft analogs of amiodarone with rapid onset and short duration of antiarrhythmic activity in guinea pigs S 19


Posters


Bodor, N.; Buchwald, P.; Ming-Ju Huang: Computer-aided retrometabolic design. Possibilities and illustrations S 20

Buchwald, P.; Bodor, N.: Molecular size based approach to estimate partition properties. Extension for peptides and peptide-CDS S 20

De Vito, S. C.: The need for the application of retrometabolic principles for the design of safer industrial chemicals S 21

Druzgala, P.; Tsou, D.;Gagné, L.; Schreier, H.: pH-activated multifunctional peptide analogs of the HA2 subunit of the influenza virus hemagglutinin: intracellular delivery through the endosomal pathway S 21

Schupke, H.; Bauer, C.; Kronbach, T.; McNeilly, P. J.; Hempel, R.; Strong, J. M.; Kupferberg, H. J.; Engel, J.: Retrometabolism by N-glucuronidation: N-glucoronides as potential shuttles for the enterohepatic circulation of amino group containing drugs ? S 22

Estes, K. S.; Dietzel, K.; Brewster, M. E.; Bodor, N.; Derendorf, H.: Rapid renal & biliary elimination of a redox-based chemical delivery sytem for estradiol in dogs S 22

Huang, F.; Ji, F.; Hochhaus, G.; Farag, H.; Browne, G.; Wu, W. M.; Bodor, N.: Receptor binding studies of soft anticholinergics S 23

Ming-Ju Huang, Tamada, S.; Hochhaus, G.; Bodor, N.: An AM1-based model for the estimation of the relative binding affinity for glucocorticoids S 23

Ji, F.; Whei-Mei Wu; Juhasz, A.; Bodor, N.: Novel soft anticholinergic agent S 24

Juhasz, A.; Wu, W. M.; Bodor, N.: Evaluation of the cardiac effects of novel soft anticholinergic compounds S 24

Ho-Seung Kim; Prokai, L.: Metabolism-based lead compound identification and optimization of neuropeptides potentially useful for treating CNS-disorders S 25

Kourounakis, A.; Galanakis, D.; Rekka, E.; Kourounakis, P.: Enhanced antioxidant and anti-inflammatory activity of cysteamine derivatives of anti-inflammatory drugs S 25

Lim, T.; Whei-Mei Wu; Bodor, N.: Retrometabolic design of drug carriers: cortienic acid derivatives and analogs as carriers with improved delivery S 26

Little, R. J.; Meccia, G.: Soft drugs based on hydrocortisone. Toward the synthesis of 17ß-chloromethyl-17-sulfonates of cortienic acid S 26

Little, R. J.; Aragort de Rossell, R.: Prodrugs of acyclic analogs of allopurinol riboside. Preliminary studies on [(2-acyloxyethoxy)methyl]-allopurinol derivatives S 27

Loftsson, T.; Bodor, N.: Percutaneous penetration of soft corticosteroids S 27

Meibohm, B.; Hochhaus, G.; Möllmann, H.; Barth, J.; Derendorf, H.: A PD/PD approach to assess the systemic activity of inhaled corticosteroids as cumulative cortisol suppression S 28

Meibohm, B.; Hochhaus, G.; Möllmann, H.; Barth, J.; Derendorf, H.: PK/PD-modeling of the circadian rhythm of the lymphocyte count in blood modulated by endogenous cortisol
S 28

Prokai-Tatrai, K.; Prokai, L.; Bodor, N.: Brain-targeting of a Leu-enkephalin analogue (dadle) by retrometabolic design S 29

Rabbani, O.; Panickar, K. S.; Rajakumar, G.; Bodor, N.; Simpkins, J. W.: Protection of cholinergic neurons using a brain-enhanced chemical delivery system for estradiol S 29

Somogyi, G.; Prokai, L.; Bodor, N.: Targeted drug delivery to the central nervous system via phosphonate derivatives S 30

Ueda, I.; Suzuki, R.; Miyawaki, K.; Kawano, T.: Design, synthesis, and radical cycloaromatization of enediyne prodrug with 1,3-butadiyne as blocking device S 30

Jiaxiang Wu; Whei-Mei Wu, Prokai, L.; Bodor, N.: Sysnthesis and pharmacological evaluation of brain-targeted chemical delivery systems of a novel TRH analog S 31

Whei-Mei Wu; Jiaxiang Wu; Prokai, L.; Bodor, N.: Effect of 2-hydroxypropyl-ß-cyclodextrin on the solubility, stability, and pharmacological activity of the chemical delivery systems of TRH analogs S 31

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