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1Author    Requires cookie*
 Title    Synthese eines Peptids m it vermutlicher W irkung des W achstum shorm on-freisetzenden Hormons (G H -R H ) A new synthesis for the tripeptide Pyr- Ser-Gly-NH2, with mutual GH-RH activity is described. Z-L-Pyr-OH is reacted with HO- NSu to the protected amino acid derivative Z-L-Pyr-ONSu. Further intermediates in the synthesis are Z-L-Pyr-L-Ser(Bzl)-OH and Z-L-Pyr-L-Ser(Bzl)-Gly-NHa  
 Abstract    Synthesis of a P eptide w ith Suggested A ctivity of G row th H orm one-R eleasing H orm one (GH-RH) K a r l Z e c h u n d W o l f g a n g V o e l t e r Peptide 
  Reference    (Z. Naturforsch. 29b, 818—819 [1974]; eingegangen am 9. Oktober 1974) 
  Published    1974 
  Keywords    hormones, Hypothalamus-releasing hormones, Peptide synthesis 
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 TEI-XML for    default:Reihe_B/29/ZNB-1974-29b-0818_n.pdf 
 Identifier    ZNB-1974-29b-0818_n 
 Volume    29 
2Author    Karl Folkers, CyrilY. Bowers, Teresa Kubiak, Janusz StepinskiRequires cookie*
 Title    Synthesis and Antiovulatory Activities in Rats of Analogs of the Luteinizing Hormone Releasing Hormone Having a Moiety of /?-(3-Quinolyl)-D-a-alanine in Positions 3 and 6  
 Abstract    Analogs of the luteinizing hormone releasing hormone (LHRH) having a moiety (D-Qal-) of/3-(3-quinolyl)-D-a-alanine were synthesized toward more effective inhibitors of ovulation. [N-Ac-^Cl-D-Phe 1 -2 , D-3-Pal 3 , D-3-Qal 6 , D-Ala 10 ]-LHRH was the most effective, and had an antiovulatory activity of 40% at 1 /ig/rat. D-3-Qal 6 was as effective as D-Trp 6 in combination with N-Ac-3 z1 Pro 1 , ^oF-D-Phe 2 , D-Trp 3 . D-Arg 6 was superior to D-3-Qal 6) in combination with N-Ac-^Cl-D-Phe 1 ' 2 , D-Trp 3 (or D-3-Pal 3), D-Ala 10 . The introduction of D-3-Qal 3 , D-His 3 and D-Arg 3 in comparable analogs caused sub-stantial loss of activities. Abbreviations D-3-Pal = /S-(3-pyridyl)-D-a-alanine; D-3-Qal = ß-(3-quinolyl)-D-a-alanine; BOC = fertf-butyloxy-carbonyl; ÄOC = tferf-amyloxycarbonyl; DCC = N,N'-dicyclohexylcarbodiimide; 3 ZlPro = 3,4-dehydro-L-proline; pF-D-Phe — yara-fluoro-D-phenylalanine; ^Cl-D-Phe = ^»am-ehloro-D-phenylalanine; Ac = acetyl, HPLC = high performance liquid chromato-graphy. 
  Reference    Z. Naturforsch. 38b, 1253—1256 (1983); received June 27 1983 
  Published    1983 
  Keywords    Ovulation, Hormone, Antagonist, Quinolylalanine, Luteinizing Hormone Releasing Hormone 
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 TEI-XML for    default:Reihe_B/38/ZNB-1983-38b-1253.pdf 
 Identifier    ZNB-1983-38b-1253 
 Volume    38 
3Author    Karl Folkers, CyrilY. Bowers, Yin-Zeng Liu, Xiao Shao-Bo, Hong-Ming Shieh, Chu Ji-YuRequires cookie*
 Title    Antagonists of the Luteinizing Hormone Releasing Hormone with Emphasis on Amino Acids in Position Five  
 Abstract    Seventeen analogs of the luteinizing hormone releasing hormone (LHRH) have been syn-thesized, bioassayed, and compared for antiovulatory activity (AOA) in rats. The emphasis of design was replacement of Tyr 5 of LHRH. Position 5 has not been extensively studied. [N—Ac—D-2-Nal 1 , D-pClPhe 2 , D-3-Pal 3 , D-Arg 6 , D—Ala 10 ]-LHRH was the baseline for new designs. Comparison of the AOA's of the 17 analogs with the baseline revealed the two peptides with Phe 5 and 3-Pal 5 had equivalent AOA's, and were the best of the 17, and about 45% more potent than the baseline. Analogs with pClPhe 5 , oClPhe 5 , a-MepClPhe 5 , 2-Nal 5 , Trp 5 , and His 5 were less potent than the Phe 5 -and 3-Pal 5 -analogs. Based on the Phe 5 -analog, eight other analogs were synthesized with changes in positions 1, 2, 3 and 7 and although none were better than the baseline, 5/8 showed 20—60% AOA's at 250 ng and revealed optimum positions for new designs. 
  Reference    Z. Naturforsch. 40b, 313—316 (1985); received August 20 1984 
  Published    1985 
  Keywords    Peptide, Hormone, Ovulation, Luteinizing Hormone Releasing Hormone, Antagonist 
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 TEI-XML for    default:Reihe_B/40/ZNB-1985-40b-0313.pdf 
 Identifier    ZNB-1985-40b-0313 
 Volume    40 
4Author    Gabriele Luckner, Paul RenzRequires cookie*
 Title    On the Phospholipase Activity in Bovine Seminal Vesicles and Its Possible Role in the Regulation of the Prostaglandin Biosynthesis  
 Abstract    A phospholipid mixture was isolated from bovine seminal vesicle tissue. This phospholipid pre­ paration contained the following prostaglandin precursor fatty acids: 4.7 percent 5,8,11-eicosa-trienoic acid, 9.1 percent 5,8,11,14-eicosatetraenoic acid and 0.9 percent 5,8,11,14,17-eicosa-pentaenoic acid. With this phospholipid preparation as substrate phospholipase activity could be detected in different fractions of bovine seminal vesicle cells. The highest phospholipase activity was found in the microsomal fraction, less in the mitochondria and essentially no activity in the cytosol. With a microsome preparation (acetone powder) of bovine seminal vesicles the influence of certain effectors on the phospholipase activity was investigated. Prostaglandins E2 and F2a (10 5 m) showed 19 and 41 percent inhibition, DB-c-AMP (2 x 10—9 m) 54 percent, c-AMP (1 0 ~ 9 m) 22 percent, epinephrine (10—4 m) 60 percent, testosterone (10—5 m) 25 percent inhibition of the phos­ pholipase activity. Whereas ethanol exhibits also a strong inhibition on the phospholipase activity, it shows a pronounced activation of the prostaglandin synthetase. 
  Reference    (Z. Naturforsch. 30c, 429 [1975]; received March 25 1975) 
  Published    1975 
  Keywords    Phospholipases, Phospholipids, Bovine Seminal Vesicles, Prostaglandins, Hormones 
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 TEI-XML for    default:Reihe_C/30/ZNC-1975-30c-0429.pdf 
 Identifier    ZNC-1975-30c-0429 
 Volume    30 
5Author    Michael Entzeroth, Lothar JaenickeRequires cookie*
 Title    Blepharisma japonicum Synthesis of Blepharismone, the Low-Molecular Conjugation Hormone of Blepharisma japonicum  
 Abstract    An effective and versatile synthesis of 5-hydroxytrypto-phane derivatives offers good access to the conjugation in­ ducing hormone blepharismone o f the ciliate Blepharisma japonicum and to derivatives and analogues of this biolog­ ically active compound. 5'-Fluoroblepharismone and 2'-des-formamidoblepharismone induce conjugation at 500 and 1200 times, respectively, the concentration of the true effector. At high concentration, however, the 2'-des-form-amido derivative desensitizes the receptor system for the natural gamone. 
  Reference    Z. Naturforsch. 36c, 180 (1981); eingegangen am 20. Oktober 1980 
  Published    1981 
  Keywords    Blepharisma japonicum, Blepharismone, Conjugation, Gamones, Hormones 
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 TEI-XML for    default:Reihe_C/36/ZNC-1981-36c-0180_n.pdf 
 Identifier    ZNC-1981-36c-0180_n 
 Volume    36 
6Author    Michael Entzeroth, Lothar JaenickeRequires cookie*
 Title    von Blepharisma japonicum Structure-Activity-Relation of Analogues and Homologues of Blepharismone, the Low-M olecular Conjugation Hormone of Blepharisma japonicum  
 Abstract    Some functional derivatives o f blepharismone, the low-m olecular conjugation hormone o f Blepharisma japonicum, were synthesised and tested for their biological activity. The lipophilicity constant o f the substituent in 5-position o f the aromatic system directly correlates with the conjugation-inducing effect o f this substance. Any change in the N -form yl-position leads to com pounds less active than blepharismone, non-active or even inhibitory. Blepharismone-related kynurenine derivatives are inhibitors o f the gamone activity depending on structural relationship. 
  Reference    Z. Naturforsch. 37c, 1136—1140 (1982); received August 2/Septem ber 20 1982 
  Published    1982 
  Keywords    Blepharisma japonicu m, Blepharismone, Conjugation, Hormones, Receptors 
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 TEI-XML for    default:Reihe_C/37/ZNC-1982-37c-1136.pdf 
 Identifier    ZNC-1982-37c-1136 
 Volume    37