Guanethidine is converted by the liver to three metabolites, which are excreted in the urine. The metabolites are pharmacologically less active than the parent compound.
来源:DrugBank
代谢
新陈代谢似乎是通过肝脏微粒体酶进行的，口服后的代谢百分比显著高于静脉给药后。
METABOLISM APPEARS TO BE BY HEPATIC MICROSOMAL ENZYMES, & PERCENTAGE METABOLIZED IS CONSIDERABLY HIGHER AFTER ORAL THAN AFTER PARENTERAL ADMIN.
来源:Hazardous Substances Data Bank (HSDB)
代谢
环状过氢氮杂环中的三级氮在人体内会显著发生N-氧化。
...TERTIARY NITROGEN OF PERHYDROAZOCINE RING UNDERGOES N-OXIDATION TO SIGNIFICANT EXTENT IN MAN.
参考文献：M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. FDA-批准的药物标签用于研究药物诱导的肝损伤，药物发现今天，16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007
M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank：按发展药物诱导人类肝损伤风险排名的最大参考药物清单。药物发现今天2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015
References:M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. FDA-Approved Drug Labeling for the Study of Drug-Induced Liver Injury, Drug Discovery Today, 16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007
M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. Drug Discov Today 2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015
...30 MIN AFTER IP ADMIN OF [(14)C]-GUANETHIDINE, ANTIHYPERTENSIVE AGENT, TO MICE, MOST OF [(14)C] WAS DISTRIBUTED IN LIVER, GI TRACT, SPLEEN, KIDNEYS, URINARY BLADDER, SALIVARY GLANDS, & BROWN FAT. IN RAT, LEVELS...IN PLASMA WERE LOWER THAN IN TISSUES...1-2 HR AFTER IP ADMIN.
HUMAN SUBJECTS RECEIVING GUANETHIDINE, HAD EXCRETED 24% OF [(14)C] IN URINE 24 HR AFTER ORAL DOSE, & 52% AFTER IV DOSE. EXCRETION OF (14)C CONTINUED, & ABOUT HALF AMT EXCRETED IN 24 HR WAS PRESENT IN URINE AFTER FURTHER 48 HR. IN 72 HR ABOUT 23% WAS EXCRETED IN FECES AFTER ORAL DOSE & 3% AFTER IV DOSE.
Amino-substituted heterocycles, compositions thereof, and methods of treatment therewith
申请人：D'Sidocky Neil R.
公开号：US20080242694A1
公开（公告）日：2008-10-02
Provided herein are Heterocyclic Compounds having the following structure:
wherein R
1
, R
2
, X, Y and Z are as defined herein, compositions comprising an effective amount of a Heterocyclic Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heterocyclic Compound to a patient in need thereof.
The present invention relates to compounds of formula I
wherein R
1
to R
4
and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
The present invention relates to compounds of formula I
wherein A and R
1
to R
4
are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
BENZOFURAN AND BENZOTHIOPHENE-2-CARBOXYLIC ACID AMIDE DERIVATIVES
申请人：Mohr Peter
公开号：US20090029976A1
公开（公告）日：2009-01-29
The present invention relates to compounds of formula I
wherein X, A and R
1
to R
4
are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia
申请人：Palani Anandan
公开号：US20060264489A1
公开（公告）日：2006-11-23
A compound having the general structure of Formula (I):
or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, wherein:
Q is selected from the group consisting of:
and
L is selected from the group consisting of:
or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome and dyslipidemia.
