Neuronorm is a potent and water soluble neurokinin A receptor antagonist

被引：3

作者：

Lombardi, A

D'Agostino, B

Filippelli, A

Pedone, C

Matera, MG

Falciani, M

De Rosa, M

Rossi, F

Pavone, V

机构：

[1] Univ Naples Federico II, Ctr Interuniveristario Ric Peptidi Bioattivi, I-90134 Palermo, Italy

[2] Univ Naples 2, Ist Biochim Macromol, I-80131 Naples, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(98)00282-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report here the synthesis and preliminary pharmacological characterization of a novel water soluble Neurokinin A receptor antagonist named Neuronorm. The synthesis was achieved in high yield by a combination of classical peptide synthesis methodologies, in both solution and solid phase. The pharmacological properties as neurokinin A receptor antagonist were assessed in in vitro experiments on rat vas deferens and guinea pig trachea, and were compared to those of MEN 10627.

引用

页码：1735 / 1740

页数：6

共 30 条

[1]

BARAN E, 1978, POL J CHEM, V52, P941

[2] NEUROPEPTIDES IN THE RESPIRATORY-TRACT .1. [J].

BARNES, PJ ;

BARANIUK, JN ;

BELVISI, MG .

AMERICAN REVIEW OF RESPIRATORY DISEASE, 1991, 144 (05) :1187-1198

[3] AMINO-ACID SEQUENCE OF SUBSTANCE P [J].

CHANG, MM ;

LEEMAN, SE ;

NIALL, HD .

NATURE-NEW BIOLOGY, 1971, 232 (29) :86-+

[4] PYBOP - A NEW PEPTIDE COUPLING REAGENT DEVOID OF TOXIC BY-PRODUCT [J].

COSTE, J ;

LENGUYEN, D ;

CASTRO, B .

TETRAHEDRON LETTERS, 1990, 31 (02) :205-208

[5]

Edmonds-Alt X, 1992, LIFE SCI, V50, P101

[6] BUILDING-BLOCKS FOR GLYCOPEPTIDE SYNTHESIS - GLYCOSYLATION OF 3-MERCAPTOPROPIONIC ACID AND FMOC AMINO-ACIDS WITH UNPROTECTED CARBOXYL GROUPS [J].

ELOFSSON, M ;

WALSE, B ;

KIHLBERG, J .

TETRAHEDRON LETTERS, 1991, 32 (51) :7613-7616

[7]

FELIX AM, 1988, INT J PEPT PROT RES, V31, P231

[8]

FILIPPELLI A, 1996, LIFE SCI, V60, P403

[9]

FOURNIER A, 1988, INT J PEPT PROT RES, V31, P86

[10] S-GLYCOSYLATED CYCLIC-PEPTIDES [J].

GERZ, M ;

MATTER, H ;

KESSLER, H .

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION IN ENGLISH, 1993, 32 (02) :269-271

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