Identification | Back Directory | [Name]
Follicle stimulating hormone | [CAS]
9002-68-0 | [EINECS(EC#)]
232-662-3 | [Molecular Formula]
NULL | [MDL Number]
MFCD00131099 |
Chemical Properties | Back Directory | [Definition]
A gonadotropic glycoprotein secreted by the anterior
pituitary gland. It regulates the metabolic activity of
the granulosa of the mammalian ovary; stimulates
maturation of ovarian follicles, and production of
estrogens. Spermatogenesis is partially under | [Appearance]
Solid; soluble in water. | [storage temp. ]
2-8°C
| [solubility ]
H2O: 50 mg/mL, soluble
| [form ]
white powder
| [Merck ]
13,4249 | [EPA Substance Registry System]
Gonadotropin, menopausal(9002-68-0) |
Questions And Answer | Back Directory | [Discovery]
This is a gonadotropic glycoprotein hormone secreted
from the anterior pituitary. FSH stimulates follicular growth
and estrogen production in the ovary and promotes spermatogenesis in the testis. In the 1960s, the purification and isolation of FSH were
reported from the ovine, porcine, bovine, and human
pituitaries. Human FSH was first fully purified in
1968. The aa sequence of the human FSH α-subunit
and its identity with the luteinizing hormone (LH)
α-subunit was demonstrated in 1974. The first aa
sequence of the FSH β-subunit was also determined in
1974. | [Structure]
FSH is a glycoprotein consisting of noncovalently
linked glycoprotein hormone (GPH) α- and FSH
β-subunits. The GPH α-subunit is common to LH,
thyroid-stimulating hormone (TSH), and chorionic
gonadotropin (CG). Both GPH α- and FSH β-subunits
contain a cysteine-knot motif, which is critical for the heterodimer assembly and biological activity of FSH. The
N- and O-linked oligosaccharide chains are important for
the intracellular folding, secretion, metabolic clearance,
and biological activity of FSH. Mr 25,000–41,000, pI 3.0–5.0. Multiple isoforms exist
due to the microheterogeneity of oligosaccharide chains.
Soluble in water, physiological saline solution, 50%
alcohol, and 50% acetone; insoluble in alcohol, acetone,
benzene, chloroform, and ether. Stable in 6 M urea; dissociated into two subunits in 1 M propionic acid. | [Gene, mRNA, and precursor]
The human GPH α-subunit gene, CGA, location 6q12-
q21, consists of four exons. Human GPH
α-subunit mRNA has 397 b that encode a signal peptide
of 24 aa residues and a mature protein of 92 aa residues. The human FSH β-subunit gene, FSHB,
location 11p13, consists of three exons.
Human FSH β-subunit mRNA has 506 b that encode a
signal peptide of 19 aa residues and a mature protein
of 110 aa residues. The GPH α- and FSH β-subunit genes are expressed in
the basophilic gonadotropes in the anterior pituitary. In
tetrapods, FSH and LH are coexpressed in gonadotropes,
whereas they are produced in different cells in teleosts. The GPH α-subunit gene is also expressed in thyrotropes
in the adenohypophysis and the placental trophoblast.
| [Synthesis and release]
The synthesis and release of FSH are regulated by
gonadotropin-releasing hormone (GnRH); gonadotropin-inhibitory hormone (GnIH); gonadal proteins such as activin, inihibin, and follistatin; and the feedback effects of
gonadal steroids.6, 7 In tetrapods, GnRH acts directly on
gonadotropes and differentially regulates FSH and LH
secretion through changes in the pattern of GnRH pulsatile
secretion. GnIH inhibits FSH secretion in birds and mammals, whereas GnIH can stimulate and inhibit FSH secretion in fish depending on the species and reproductive
status. Activin stimulates FSH secretion through binding
to the activin receptor at the cell membrane of the gonadotropes, which is antagonized by the binding of inhibin and
follistatin. FSH secretion is also regulated by gonadal
steroids such as estradiol and progesterone. Gonadal steroids exert their effects at the level of the hypothalamus
by changing GnRH secretion; and directly at the level of
the gonadotropes, where they exert different effects,
depending on the species and reproductive condition of
the animals. | [Receptors]
The receptor of FSH (FSHR) is a glycoprotein that
belongs to a subclass of the rhodopsin/β-adrenergic
subfamily of the membrane-bound GPCR superfamily. The human FSHR gene, FSHR, location 2p16.3, consists of
10 exons. The FSHR consists of 650–700 aa residues that contain a large N-terminal extracellular domain
(~350 aa residues), seven transmembrane domains, and a
C-terminal intracellular domain. The receptor mainly couples to the Gs protein, and
FSH stimulates the production of cAMP in target cells. | [Agonists and Antagonists]
Purified and recombinant human FSH, thiazolidinone
compounds, cyclic and acyclic α- and β-aminocarboxamide
derivatives, and biaryl derivatives are agonists. Antibodies to FSHR, aminoalkylamide derivatives, tetrahydroquinoline derivatives, 7-{4-[bis-(2-carbamoyl-ethyl)-
amino]-6-chloro-(1,3,5)-triazin-2-ylamino)-4-hydroxy-3-(4-
methoxy-phenylazo)-naphthalene}-2-sulfonic acid, and suramin (a nonselective FSHR-antagonist) are antagonists. | [Clinical implications]
Hypergonadotropic ovarian dysgenesis is a disease
characterized by a normal karyotype, highly elevated
gonadotropins, and streaky gonads associated with primary amenorrhea. A mutation (Ala 189 Val) in the extracellular domain of FSHR is considered a probable cause
of the disease. Functional studies revealed a lack of
cAMP production by the mutated receptor upon FSH
stimulation. FSH levels are useful in the investigation
of menstrual irregularities, and in the diagnosis of pituitary disorders or diseases involving the ovaries or testes.
Conditions with high FSH levels include premature menopause (i.e., premature ovarian failure), poor ovarian
reserve, gonadal dysgenesis, Turner syndrome, Swyer
syndrome, and Klinefelter syndrome. Conditions with
low FSH levels include hypopituitarism, polycystic ovarian syndrome, Kallmann syndrome, Sheehan syndrome,
and Chiari-Frommel syndrome. |
Hazard Information | Back Directory | [Chemical Properties]
Solid; soluble in water. | [Uses]
A major gonadotropin secreted by the adenohypophysis (PITUITARY GLAND, ANTERIOR). Follicle-stimulating hormone stimulates GAMETOGENESIS and the supporting cells such as the ovarian GRANULOSA CELLS, the testicular SERTOLI CELLS, and LEYDIG CELLS. FSH consi | [Brand name]
Humegon (Organon); Pergonal (Serono). |
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