STEARYL-NORLEUCINE-VASOACTIVE INTESTINAL PEPTIDE (VIP) - A NOVEL VIP ANALOG FOR NONINVASIVE IMPOTENCE TREATMENT

被引:45
作者
GOZES, I [1 ]
RESHEF, A [1 ]
SALAH, D [1 ]
RUBINRAUT, S [1 ]
FRIDKIN, M [1 ]
机构
[1] WEIZMANN INST SCI, DEPT ORGAN CHEM, REHOVOT, ISRAEL
关键词
D O I
10.1210/en.134.5.2121
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
The present report relates to pharmaceutical composition for the treatment of male impotence. The transdermal application of a potent derivative of vasoactive intestinal peptide (VIP) coupled to a suitable hydrophobic moiety (e.g. stearyl-VIP) in a suitable ointment composition (e.g. Sefsol) enhances sexual activity and erection formation in a variety of impotence models in rats (sterile rats, diabetic rats, and animals with high blood pressure). Furthermore, exchange of the methionine in position 17 with norleucine enhances biological activity. Thus, stearyl-Nle(17)-VIP may be considered useful for the treatment of impotence.
引用
收藏
页码:2121 / 2125
页数:5
相关论文
共 23 条
[1]   IS VASOACTIVE INTESTINAL POLYPEPTIDE THE PRINCIPAL TRANSMITTER INVOLVED IN HUMAN PENILE ERECTION [J].
ADAIKAN, PG ;
KOTTEGODA, SR ;
RATNAM, SS .
JOURNAL OF UROLOGY, 1986, 135 (03) :638-640
[2]   HEMODYNAMICS OF PELVIC NERVE INDUCED PENILE ERECTION IN THE DOG - POSSIBLE MEDIATION BY VASOACTIVE INTESTINAL POLYPEPTIDE [J].
ANDERSSON, PO ;
BLOOM, SR ;
MELLANDER, S .
JOURNAL OF PHYSIOLOGY-LONDON, 1984, 350 (MAY) :209-224
[3]   VIP-MESSENGER RNA IS INCREASED IN HYPERTENSIVE RATS [J].
AVIDOR, R ;
EILAM, R ;
MALACH, R ;
GOZES, I .
BRAIN RESEARCH, 1989, 503 (02) :304-307
[4]  
BENSON GS, 1981, INVEST UROL, V19, P65
[5]  
BINDLEY GS, 1983, BRIT J PSYCHIAT, V143, P332
[6]   VASOACTIVE INTESTINAL POLYPEPTIDE-LIKE IMMUNOREACTIVE NERVES IN DIABETIC PENIS - A COMPARISON BETWEEN STREPTOZOTOCIN-TREATED RATS AND MAN [J].
CROWE, R ;
LINCOLN, J ;
BLACKLAY, PF ;
PRYOR, JP ;
LUMLEY, JSP ;
BURNSTOCK, G .
DIABETES, 1983, 32 (11) :1075-1077
[7]   EFFECTS OF TACTILE AND ELECTRICAL STIMULI UPON RELEASE OF VASOACTIVE INTESTINAL POLYPEPTIDE IN THE MAMMALIAN PENIS [J].
DIXSON, AF ;
KENDRICK, KM ;
BLANK, MA ;
BLOOM, SR .
JOURNAL OF ENDOCRINOLOGY, 1984, 100 (02) :249-252
[8]  
FAUCHERE JL, 1988, INT J PEPT PROT RES, V32, P268
[9]   VIP - MOLECULAR-BIOLOGY AND NEUROBIOLOGICAL FUNCTION [J].
GOZES, I ;
BRENNEMAN, DE .
MOLECULAR NEUROBIOLOGY, 1989, 3 (04) :201-236
[10]   A FATTY NEUROPEPTIDE - POTENTIAL-DRUG FOR NONINVASIVE IMPOTENCE TREATMENT IN A RAT MODEL [J].
GOZES, I ;
FRIDKIN, M .
JOURNAL OF CLINICAL INVESTIGATION, 1992, 90 (03) :810-814