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This article is about gonadorelin (GnRH) as a medication. For its role as a hormone, see
GnRH .
Gonadorelin Trade names Factrel, HRF, Kryptocur, Lutrelef, Lutrepulse, Relefact, others Other names Abbott 41070; AY-24031; Hoe-471; RU-19847 Routes of intravenous , subcutaneous [1] Drug class GnRH analogue ; GnRH agonist ; Progonadotropin ATC code
Legal status Metabolism Hydrolysis [1] Elimination half-life 10–40 minutes[1]
(2 S N 2 S 2 S 2 S 2 S 2 S 2 S 2 S 1 H 1 H
CAS Number PubChem CID DrugBank ChemSpider UNII KEGG ChEBI ChEMBL CompTox Dashboard (EPA ) ECHA InfoCard 100.046.852 Formula C 55 H 75 N 17 O 13 Molar mass 1 182 .311−1 3D model (JSmol )
CC(C )C[C@@H](C(=O)N[C@@H](CCCN=C(N )N)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N)NC(=O)CNC(=O)[C@H](CC2=CC=C(C=C2)O)NC(=O)[C@H](CO )NC(=O)[C@H](CC3=CNC4=CC=CC=C43)NC(=O)[C@H](CC5=CN=CN5)NC(=O)[C@@H]6CCC(=O)N6
InChI=1S/C55H75N17O13/c1-29(2 )19-38(49(80 )67-37(9-5-17-60-55(57 )58)54(85 )72-18-6-10-43(72 )53(84 )62-25-44(56 )75)66-46(77 )26-63-47(78 )39(20-30-11-13-33(74 )14-12-30)68-52(83 )42(27-73)71-50(81 )40(21-31-23-61-35-8-4-3-7-34(31 )35)69-51(82 )41(22-32-24-59-28-64-32)70-48(79 )36-15-16-45(76 )65-36/h3-4,7-8,11-14,23-24,28-29,36-43,61,73-74H,5-6,9-10,15-22,25-27H2,1-2H3,(H2,56,75)(H,59,64)(H,62,84)(H,63,78)(H,65,76)(H,66,77)(H,67,80)(H,68,83)(H,69,82)(H,70,79)(H,71,81)(H4,57,58,60)/t36-,37-,38-,39-,40-,41-,42-,43-/m0/s1
Key:XLXSAKCOAKORKW-AQJXLSMYSA-N
Gonadorelin is a gonadotropin-releasing hormone agonist (GnRH agonist) which is used in fertility medicine and to treat amenorrhea and hypogonadism .[2] [3] [4] [5] [6] [7] veterinary medicine .[3] [5] endogenous GnRH and is identical to it in chemical structure .[2] [3] [5] [7] injection into a blood vessel or fat or as a nasal spray .[5] [1] [7]
Medical uses [ edit ]
Gonadorelin is used as a diagnostic agent to assess pituitary gland function.[1] primary hypothalamic amenorrhea , hypogonadotropic hypogonadism (e.g., Kallmann syndrome ), delayed puberty , cryptorchidism , and infertility .[7] [8] [1] [9]
Available forms [ edit ]
Gonadorelin is available in a portable infusion pump that provides pulsatile subcutaneous administration of the drug.[7] [8] [7] [8] solution form for intravenous or subcutaneous injection and as a nasal spray .[7]
Pharmacology [ edit ]
Pharmacodynamics [ edit ]
Gonadorelin is an agonist of the GnRH receptor and is used to induce the secretion of the gonadotropins follicle-stimulating hormone and luteinizing hormone from the pituitary gland and to increase sex hormone production by the gonads .[7] [8]
Pharmacokinetics [ edit ]
Gonadorelin has a distribution half-life of 2 to 10 minutes and a very short terminal half-life of 10 to 40 minutes.[1] metabolized by hydrolysis into smaller peptide components.[1]
History [ edit ]
Gonadorelin was available for medical use, under the brand name Factrel, as early as 1978.[10]
Society and culture [ edit ]
Generic names [ edit ]
Gonadorelin is the generic name of the drug and its INN Tooltip International Nonproprietary Name , BAN Tooltip British Approved Name , and JAN Tooltip Japanese Accepted Name , while gonadorelina is its DCIT Tooltip Denominazione Comune Italiana and gonadoréline is its DCF Tooltip Dénomination Commune Française . The diacetate salt is known as gonadorelin acetate and this is its USAN Tooltip United States Adopted Name , BANM Tooltip British Approved Name , and JAN Tooltip Japanese Accepted Name , while the hydrochloride salt is known as gonadorelin hydrochloride and this is its USAN Tooltip United States Adopted Name and BANM Tooltip British Approved Name .[2] [3] [5]
Brand names [ edit ]
Free alcohol gonadorelin has been marketed under the brand names Cryptocur, Cystoréline, Fertagyl, GnRH Serono, Gonadorelin, HRF, Kryptocur, LH-RH, Luforan, Pulstim, Relefact, Relisorm L, Stimu-LH, and Wyeth-Ayest HRF.[3] [5] [3] [5] [3] [5] [5] [3] [5]
Availability [ edit ]
Gonadorelin is available widely throughout the world for veterinary use, including in the United States , Canada , the United Kingdom , Ireland , elsewhere throughout Europe , South Africa , Australia , New Zealand , Japan , Taiwan , and in many other countries.[3] [5] [11] United States .[12]
See also [ edit ]
References [ edit ]
^ a b c d e f g h i Index Nominum 2000: International Drug Directory ISBN 978-3-88763-075-1
^ Morton IK, Hall JM (6 December 2012). Concise Dictionary of Pharmacological Agents: Properties and Synonyms ISBN 978-94-011-4439-1
^ a b c d e f g h i j k "Gonadorelin injectable Uses, Side Effects & Warnings" .
^ Shao WM, Bai WJ, Chen YM, Liu L, Wang YJ (August 2014). "[Micropump infusion of gonadorelin in the treatment of hypogonadotropic hypogonadism in patients with pituitary stalk interruption syndrome: cases analysis and literature review]". Beijing da Xue Xue Bao. Yi Xue Ban = Journal of Peking University. Health Sciences (in Chinese). 46 4 ): 642–645. PMID 25131486 .
^ a b c d e f g h Köhn FM, Schill WB (17 July 2017). "Hormone Substitution in Male Infertility" . In Allahbadia GN, Chawla MM, Das RB, Garcia EV, Gandhi G, Merchant R (eds.). The Art & Science of Assisted Reproductive Techniques (ART) . JP Medical Ltd. pp. 731–. ISBN 978-93-86322-82-1
^ a b c d Mokotoff M (2002). "Peptide and Protein Drugs" . In Williams DA, Foye WO, Lemke TL (eds.). Foye's Principles of Medicinal Chemistry . Lippincott Williams & Wilkins. pp. 128–. ISBN 978-0-683-30737-5
^ Goodman LS, Gilman AD (January 1996). Goodman & Gilman's the Pharmacological Basis of Therapeutics ISBN 978-0-07-026266-9
^ Bain J, Moskowitz JP, Clapp JJ (1978). "LH and FSH response to gonadotropin releasing hormone (GnRH) in normospermic, oligospermic and azoospermic men". Archives of Andrology . 1 2 ): 147–152. doi :10.3109/01485017808988331 . PMID 367302 .
^ Sweetman SC, ed. (2009). "Sex hormones and their modulators" . Martindale: The Complete Drug Reference (36th ed.). London: Pharmaceutical Press. pp. 2106–2108. ISBN 978-0-85369-840-1
^ "Drugs@FDA: FDA-Approved Drugs" . FDA.gov . Retrieved 30 December 2021 .
t
e
GnRH modulatorsanalogues )
Gonadotropins
Others
Progonadotropins
Antigonadotropins
Sex steroid agonists (via negative feedback on the HPG axis Androgens /anabolic steroids (e.g., testosterone , nandrolone esters , oxandrolone )
D 2 antagonists (prolactin releasers ) (incl., domperidone , metoclopramide , risperidone , haloperidol , chlorpromazine , sulpiride )
Estrogens (incl., bifluranol , estradiol , estradiol esters , ethinylestradiol , diethylstilbestrol , paroxypropione )
Progestogens (incl. progestins , e.g., chlormadinone acetate , cyproterone acetate , hydroxyprogesterone caproate , gestonorone caproate , medroxyprogesterone acetate , megestrol acetate )
Clinical trials :
See also
GnRH and gonadotropin receptor modulators
Androgens and antiandrogens
Estrogens and antiestrogens
Progestogens and antiprogestogens
t
e
GnRH Tooltip Gonadotropin-releasing hormone receptor
Gonadotropin
LH/hCG Tooltip Luteinizing hormone/choriogonadotropin receptor
FSH Tooltip Follicle-stimulating hormone receptor
R e t r i e v e d f r o m " https://en.wikipedia.org/w/index.php?title=Gonadorelin&oldid=1187604382 " C a t e g o r i e s : ● G n R H a g o n i s t s ● P e p t i d e s ● P r o g o n a d o t r o p i n s ● V e t e r i n a r y d r u g s H i d d e n c a t e g o r i e s : ● C S 1 C h i n e s e - l a n g u a g e s o u r c e s ( zh ) ● A r t i c l e s w i t h s h o r t d e s c r i p t i o n ● S h o r t d e s c r i p t i o n m a t c h e s W i k i d a t a ● E C H A I n f o C a r d I D f r o m W i k i d a t a ● A r t i c l e s c o n t a i n i n g u n v e r i f i e d c h e m i c a l i n f o b o x e s
● T h i s p a g e w a s l a s t e d i t e d o n 3 0 N o v e m b e r 2 0 2 3 , a t 0 7 : 5 5 ( U T C ) . ● T e x t i s a v a i l a b l e u n d e r t h e C r e a t i v e C o m m o n s A t t r i b u t i o n - S h a r e A l i k e L i c e n s e 4 . 0 ;
a d d i t i o n a l t e r m s m a y a p p l y . B y u s i n g t h i s s i t e , y o u a g r e e t o t h e T e r m s o f U s e a n d P r i v a c y P o l i c y . W i k i p e d i a ® i s a r e g i s t e r e d t r a d e m a r k o f t h e W i k i m e d i a F o u n d a t i o n , I n c . , a n o n - p r o f i t o r g a n i z a t i o n . ● P r i v a c y p o l i c y ● A b o u t W i k i p e d i a ● D i s c l a i m e r s ● C o n t a c t W i k i p e d i a ● C o d e o f C o n d u c t ● D e v e l o p e r s ● S t a t i s t i c s ● C o o k i e s t a t e m e n t ● M o b i l e v i e w
