PTR-3046(PTR-3046) - 药物靶点：SSTR_专利_临床

概要

基本信息

药物类型

合成多肽

别名

靶点

SSTR

作用机制

SSTR拮抗剂(生长抑素受体拮抗剂)

治疗领域

消化系统疾病

在研适应症-

非在研适应症

胰腺炎

原研机构

Peptor Ltd

在研机构-

非在研机构

Peptor Ltd

Yissum Research Development Co. Ltd.

最高研发阶段终止临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C59H77N11O10

InChIKeyLRUHWPFUOBQIRY-OHMZANSPSA-N

CAS号203200-47-9

序列信息

Sequence Code 319911343

关联

100 项与 PTR-3046 相关的临床结果

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100 项与 PTR-3046 相关的转化医学

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100 项与 PTR-3046 相关的专利（医药）

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1

项与 PTR-3046 相关的文献（医药）

1998-03-01·Journal of Medicinal Chemistry1区 · 医学

A Backbone-Cyclic, Receptor 5-Selective Somatostatin Analogue: Synthesis, Bioactivity, and Nuclear Magnetic Resonance Conformational Analysis

1区 · 医学

Article

作者: Arad, Oded ; Wanger, Mazal ; Huenges, Martin ; Kessler, Horst ; Gellerman, Gary ; Feller, Etty ; Ziv, Ofer ; Afargan, Michel ; Gamliel, Asher ; Amitay, Oved ; Mathä, Barbara ; Gilon, Chaim ; Shohat, Dvira ; Hornik, Vered

Cyclo(PheN2-Tyr-D-Trp-Lys-Val-PheC3)-Thr-NH2 (PTR 3046), a backbone-cyclic somatostatin analogue, was synthesized by solid-phase methodology. The binding characteristics of PTR 3046 to the different somatostatin receptors, expressed in CHO cells, indicate high selectivity to the SSTR5 receptor. PTR 3046 is highly stable against enzymatic degradation as determined in vitro by incubation with rat renal homogenate and human serum. The biological activity of PTR 3046 in vivo was determined in rats. PTR 3046 inhibits bombesin- and caerulein-induced amylase and lipase release from the pancreas without inhibiting growth hormone or glucagon release. The major conformation of PTR 3046 in CD3OH, as determined by NMR, is defined by a type II' beta-turn at D-Trp-Lys and a cis amide bond at Val-PheC3.

100 项与 PTR-3046 相关的药物交易

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