lhrh, n-ac-2-nal(1)-4-cl-phe(2)-trp(3)-hci(6)-alanh2(10)- profile

LHRH, N-Ac-2-Nal(1)-4-Cl-Phe(2)-Trp(3)-Hci(6)-AlaNH2(10)-: RN given refers to (D-Ala-D-Phe-D-Trp-L-Ser-L-Tyr-D-Lys-L-Leu-L-Arg-L-Pro-D-Ala)-isomer; RN for cpd without isomeric designation not avail 10/90; LHRH antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	16157681
MeSH ID	M0180860

Synonym
sb-29
unii-1m0mso61ea
gnrh, n-ac-2-nal(1)-4-cl-phe(2)-trp(3)-hci(6)-alanh2(10)-
d-alaninamide, n-acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-d-tryptophyl-l-seryl-l-tyrosyl-n6-(aminocarbonyl)-d-lysyl-l-leucyl-l-arginyl-l-prolyl-
lhrh, n-acetyl-2-naphthalenylalanyl(1)-4-chlorophenylalanyl(2)-tryptophyl(3)-homocitrullinyl(6)-alaninamide(10)-
1m0mso61ea ,
lhrh, n-ac-2-nal(1)-4-cl-phe(2)-trp(3)-hci(6)-alanh2(10)-
n-ac-1-(2-nal)-2-(4-cl-phe)-3-trp-6-hci-10-alanh2-lhrh
lhrh, n-ac-2-nal(1)-4-cl-phe(2)-3-pal(3)-arg(5)-glu(6)-alanh2(10)-
lhrh, n-ac-2-nal(1)-4-cl-phe(2)-trp(3)-d-homocitrulline(6)-alanh2(10)-

Excerpt	Reference	Relevance
" In the subchronic study, all doses of Nal-Glu were well tolerated and there were no apparent systemic toxic effects."	( A 90-day subcutaneous toxicity and fertility study of a LHRH antagonist in rats. Bardin, CW; DeJesus, W; Didolkar, AK; Keizer-Zucker, A; Rivier, J; Sundaram, K; Vale, W, 1990)	0.28

Excerpt	Reference	Relevance
"We administered Nal-Glu at doses of 0, 100, and 200 micrograms/kg body weight per day in combination with T enanthate, 50 mg IM weekly, to separate groups of men (9 or 10 men per group) for 4 weeks."	( Dose effects of the gonadotropin-releasing hormone antagonist, Nal-Glu, combined with testosterone enanthate on gonadotropin levels in normal men. Bagatell, CJ; Bremner, WJ; Rivier, JE, 1995)	0.29
"Administration of Nal-Glu in combination with T suppresses gonadotropins more completely than does T alone, but at doses > 100 micrograms/kg, gonadotropins are not suppressed additionally with larger doses of Nal-Glu."	( Dose effects of the gonadotropin-releasing hormone antagonist, Nal-Glu, combined with testosterone enanthate on gonadotropin levels in normal men. Bagatell, CJ; Bremner, WJ; Rivier, JE, 1995)	0.29

Excerpt	Relevance	Reference
"The dose-response effects of a single administration of Nal-Lys-GnRHant (antagonist) on serum LH and FSH concentrations were compared to the effects of Nal-Glu-GnRHant in monkeys."	( Prolonged duration of gonadotropin inhibition by a third generation GnRH antagonist. Danforth, DR; Gordon, K; Hodgen, GD; Leal, JA; Williams, RF, 1988)	0.27
" Using a placental explant culture system, a dose-response effect of hCG secretion was observed in the placental explant at 9 weeks when treated with GnRH ranging from 10(-9)-10(-7) mol/L."	( Expression of human gonadotropin-releasing hormone receptor gene in the placenta and its functional relationship to human chorionic gonadotropin secretion. Lin, LS; Roberts, VJ; Yen, SS, 1995)	0.29

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	7 (8.75)	18.7374
1990's	71 (88.75)	18.2507
2000's	0 (0.00)	29.6817
2010's	2 (2.50)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	14 (16.87%)	5.53%
Reviews	1 (1.20%)	6.00%
Case Studies	1 (1.20%)	4.05%
Observational	0 (0.00%)	0.25%
Other	67 (80.72%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
histamine [no description available]	1.97	1	0	aralkylamino compound; imidazoles	human metabolite; mouse metabolite; neurotransmitter
flutamide Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species.	2.39	2	0	(trifluoromethyl)benzenes; monocarboxylic acid amide	androgen antagonist; antineoplastic agent
activins Activins: Activins are produced in the pituitary, gonads, and other tissues. By acting locally, they stimulate pituitary FSH secretion and have diverse effects on cell differentiation and embryonic development. Activins are glycoproteins that are hetero- or homodimers of INHIBIN-BETA SUBUNITS.	1.98	1	0
procarbazine Procarbazine: An antineoplastic agent used primarily in combination with mechlorethamine, vincristine, and prednisone (the MOPP protocol) in the treatment of Hodgkin's disease.. procarbazine : A benzamide obtained by formal condensation of the carboxy group of 4-[(2-methylhydrazino)methyl]benzoic acid with the amino group of isopropylamine. An antineoplastic chemotherapy drug used for treatment of Hodgkin's lymphoma. Metabolism yields azo-procarbazine and hydrogen peroxide, which results in the breaking of DNA strands.	1.98	1	0	benzamides; hydrazines	antineoplastic agent
estrone Hydroxyestrones: Estrone derivatives substituted with one or more hydroxyl groups in any position. They are important metabolites of estrone and other estrogens.	1.98	1	0	17-oxo steroid; 3-hydroxy steroid; phenolic steroid; phenols	antineoplastic agent; bone density conservation agent; estrogen; human metabolite; mouse metabolite
ethinyl estradiol Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.. 17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration.	1.98	1	0	17-hydroxy steroid; 3-hydroxy steroid; terminal acetylenic compound	xenoestrogen
androstenedione Androstenedione: A delta-4 C19 steroid that is produced not only in the TESTIS, but also in the OVARY and the ADRENAL CORTEX. Depending on the tissue type, androstenedione can serve as a precursor to TESTOSTERONE as well as ESTRONE and ESTRADIOL.. androst-4-ene-3,17-dione : A 3-oxo Delta(4)-steroid that is androst-4-ene substituted by oxo groups at positions 3 and 17. It is a steroid hormone synthesized in the adrenal glands and gonads.	1.98	1	0	17-oxo steroid; 3-oxo-Delta(4) steroid; androstanoid	androgen; Daphnia magna metabolite; human metabolite; mouse metabolite
norethindrone Norethindrone: A synthetic progestational hormone with actions similar to those of PROGESTERONE but functioning as a more potent inhibitor of ovulation. It has weak estrogenic and androgenic properties. The hormone has been used in treating amenorrhea, functional uterine bleeding, endometriosis, and for CONTRACEPTION.. norethisterone : A 17beta-hydroxy steroid that is testosterone in which the hydrogen at position 17 is replaced by an ethynyl group and in which the methyl group attached to position 10 is replaced by hydrogen.	1.98	1	0	17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound; tertiary alcohol	progestin; synthetic oral contraceptive
pregnenolone [no description available]	1.98	1	0	20-oxo steroid; 3beta-hydroxy-Delta(5)-steroid; C21-steroid	human metabolite; mouse metabolite
testosterone enanthate [no description available]	6.23	4	2	heptanoate ester; sterol ester	androgen
nandrolone Nandrolone: C18 steroid with androgenic and anabolic properties. It is generally prepared from alkyl ethers of ESTRADIOL to resemble TESTOSTERONE but less one carbon at the 19 position.. nandrolone : A 3-oxo Delta(4)-steroid that is estr-4-en-3-one substituted by a beta-hydroxy group at position 17.	2.08	1	0	17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; anabolic androgenic steroid	human metabolite
testolactone Testolactone: An antineoplastic agent that is a derivative of progesterone and used to treat advanced breast cancer.	3.37	1	1	3-oxo-Delta(1),Delta(4)-steroid; seco-androstane
buserelin Buserelin: A potent synthetic analog of GONADOTROPIN-RELEASING HORMONE with D-serine substitution at residue 6, glycine10 deletion, and other modifications.	2.38	2	0	oligopeptide
mifepristone Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME.	3.36	1	1	3-oxo-Delta(4) steroid; acetylenic compound; tertiary amino compound	abortifacient; contraceptive drug; hormone antagonist; synthetic oral contraceptive
fura-2 Fura-2: A fluorescent calcium chelating agent which is used to study intracellular calcium in tissues.	1.98	1	0
estradiol 3-benzoate 17beta-estradiol 3-benzoate : A benzoate ester resulting from the formal condensation of benzoic acid with the phenolic hydroxy group of 17beta-estradiol.	1.98	1	0	17beta-hydroxy steroid; benzoate ester	estrogen receptor agonist; xenoestrogen
n-acetylneuraminic acid N-Acetylneuraminic Acid: An N-acyl derivative of neuraminic acid. N-acetylneuraminic acid occurs in many polysaccharides, glycoproteins, and glycolipids in animals and bacteria. (From Dorland, 28th ed, p1518). N-acetylneuraminic acid : An N-acylneuraminic acid where the N-acyl group is specified as acetyl.	3.44	1	1	N-acetylneuraminic acids	antioxidant; bacterial metabolite; EC 3.2.1.18 (exo-alpha-sialidase) inhibitor; human metabolite; mouse metabolite
leuprolide Leuprolide: A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE that regulates the synthesis and release of pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE.. leuprolide : An oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, D-leucyl, leucyl, arginyl, and N-ethylprolinamide residues joined in sequence. It is a synthetic nonapeptide analogue of gonadotropin-releasing hormone, and is used as a subcutaneous hydrogel implant (particularly as the acetate salt) for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.	3.08	5	0	oligopeptide	anti-estrogen; antineoplastic agent; gonadotropin releasing hormone agonist
enclomiphene Enclomiphene: The trans or (E)-isomer of clomiphene.	1.98	1	0
trestolone trestolone: structure given in first source; RN given refers to (7alpha,17beta)-isomer	2.08	1	0
calcimycin Calcimycin: An ionophorous, polyether antibiotic from Streptomyces chartreusensis. It binds and transports CALCIUM and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems.	1.98	1	0	benzoxazole
detirelix detirelix: LHRH antagonist	1.98	1	0
iturelix iturelix: a gonadotropin-releasing hormone antagonist	2.67	3	0
azaline azaline: gonadorelin antagonist; RN & amino acid sequence given in first source	1.98	1	0
menotropins Menotropins: Extracts of urine from menopausal women that contain high concentrations of pituitary gonadotropins, FOLLICLE STIMULATING HORMONE and LUTEINIZING HORMONE. Menotropins are used to treat infertility. The FSH:LH ratio and degree of purity vary in different preparations.	4.62	6	1
lhrh, ac-dehydro-pro(1)-4-f-phe(2)-trp(3,6)- LHRH, Ac-dehydro-Pro(1)-4-F-Phe(2)-Trp(3,6)-: RN given refers to (L-Pro-D-Phe-D-Trp-D-Trp)-isomer; LHRH antagonist	1.98	1	0
trelstar Triptorelin Pamoate: A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE with D-tryptophan substitution at residue 6.	2.38	2	0
cetrorelix cetrorelix: LHRH antagonist. cetrorelix : A synthetic ten-membered oligopeptide comprising N-acetyl-3-(naphthalen-2-yl)-D-alanyl, 4-chloro-D-phenylalanyl, 3-(pyridin-3-yl)-D-alanyl, L-seryl, L-tyrosyl, N(5)-carbamoyl-D-ornithyl, L-leucyl, L-arginyl, L-prolyl, and D-alaninamide residues coupled in sequence. A gonadotrophin-releasing hormone (GnRH) antagonist, it is used for treatment of infertility and of hormone-sensitive cancers of the prostate and breast.	1.98	1	0	oligopeptide	antineoplastic agent; GnRH antagonist

Condition	Relationship Strength	Studies	Trials
Breast Cancer [description not available]	1.97	1	0
Breast Neoplasms Tumors or cancer of the human BREAST.	1.97	1	0
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	4.06	3	1
Anaphylactic Reaction [description not available]	1.98	1	0
Anaphylaxis An acute hypersensitivity reaction due to exposure to a previously encountered ANTIGEN. The reaction may include rapidly progressing URTICARIA, respiratory distress, vascular collapse, systemic SHOCK, and death.	1.98	1	0
Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.	3.08	5	0
Adenoma, Basal Cell [description not available]	4.28	4	1
Cancer of Pituitary [description not available]	4.28	4	1
Ovarian Hyperstimulation Syndrome, Familial Gestational Spontaneous [description not available]	2.38	2	0
Adenoma A benign epithelial tumor with a glandular organization.	4.28	4	1
Pituitary Neoplasms Neoplasms which arise from or metastasize to the PITUITARY GLAND. The majority of pituitary neoplasms are adenomas, which are divided into non-secreting and secreting forms. Hormone producing forms are further classified by the type of hormone they secrete. Pituitary adenomas may also be characterized by their staining properties (see ADENOMA, BASOPHIL; ADENOMA, ACIDOPHIL; and ADENOMA, CHROMOPHOBE). Pituitary tumors may compress adjacent structures, including the HYPOTHALAMUS, several CRANIAL NERVES, and the OPTIC CHIASM. Chiasmal compression may result in bitemporal HEMIANOPSIA.	4.28	4	1
Ovarian Hyperstimulation Syndrome A complication of OVULATION INDUCTION in infertility treatment. It is graded by the severity of symptoms which include OVARY enlargement, multiple OVARIAN FOLLICLES; OVARIAN CYSTS; ASCITES; and generalized EDEMA. The full-blown syndrome may lead to RENAL FAILURE, respiratory distress, and even DEATH. Increased capillary permeability is caused by the vasoactive substances, such as VASCULAR ENDOTHELIAL GROWTH FACTORS, secreted by the overly-stimulated OVARIES.	2.38	2	0
Sterility, Female [description not available]	1.98	1	0
Infertility, Female Diminished or absent ability of a female to achieve conception.	1.98	1	0
Polycystic Ovarian Syndrome [description not available]	4.06	3	1
Polycystic Ovary Syndrome A complex disorder characterized by infertility, HIRSUTISM; OBESITY; and various menstrual disturbances such as OLIGOMENORRHEA; AMENORRHEA; ANOVULATION. Polycystic ovary syndrome is usually associated with bilateral enlarged ovaries studded with atretic follicles, not with cysts. The term, polycystic ovary, is misleading.	4.06	3	1
Hyperandrogenism A condition caused by the excessive secretion of ANDROGENS from the ADRENAL CORTEX; the OVARIES; or the TESTES. The clinical significance in males is negligible. In women, the common manifestations are HIRSUTISM and VIRILISM as seen in patients with POLYCYSTIC OVARY SYNDROME and ADRENOCORTICAL HYPERFUNCTION.	1.98	1	0
Aggression Behavior which may be manifested by destructive and attacking action which is verbal or physical, by covert attitudes of hostility or by obstructionism.	4.69	2	1
Hematuria Presence of blood in the urine.	1.98	1	0
Libman-Sacks Disease [description not available]	1.98	1	0
Lupus Erythematosus, Systemic A chronic, relapsing, inflammatory, and often febrile multisystemic disorder of connective tissue, characterized principally by involvement of the skin, joints, kidneys, and serosal membranes. It is of unknown etiology, but is thought to represent a failure of the regulatory mechanisms of the autoimmune system. The disease is marked by a wide range of system dysfunctions, an elevated erythrocyte sedimentation rate, and the formation of LE cells in the blood or bone marrow.	1.98	1	0
Proteinuria The presence of proteins in the urine, an indicator of KIDNEY DISEASES.	1.98	1	0
Hypospermatogenesis [description not available]	5.44	3	1
Weight Gain Increase in BODY WEIGHT over existing weight.	4.28	1	1
Fibroid [description not available]	3.37	1	1
Cancer of the Uterus [description not available]	3.37	1	1
Flushing A transient reddening of the face that may be due to fever, certain drugs, exertion, or stress.	3.37	1	1
Leiomyoma A benign tumor derived from smooth muscle tissue, also known as a fibroid tumor. They rarely occur outside of the UTERUS and the GASTROINTESTINAL TRACT but can occur in the SKIN and SUBCUTANEOUS TISSUE, probably arising from the smooth muscle of small blood vessels in these tissues.	3.37	1	1
Uterine Neoplasms Tumors or cancer of the UTERUS.	3.37	1	1
Menopause The last menstrual period. Permanent cessation of menses (MENSTRUATION) is usually defined after 6 to 12 months of AMENORRHEA in a woman over 45 years of age. In the United States, menopause generally occurs in women between 48 and 55 years of age.	3.07	5	0
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	1.98	1	0
Atrophy Decrease in the size of a cell, tissue, organ, or multiple organs, associated with a variety of pathological conditions such as abnormal cellular changes, ischemia, malnutrition, or hormonal changes.	1.97	1	0
Ectopic Hormone Syndromes [description not available]	1.97	1	0
Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.	1.97	1	0

lhrh, n-ac-2-nal(1)-4-cl-phe(2)-trp(3)-hci(6)-alanh2(10)-

Description

Cross-References

Synonyms (10)

Research Excerpts

Toxicity

Compound-Compound Interactions

Dosage Studied

Research

Studies (80)

Study Types