Would drugs that block cell receptors for FSH be useful in males and/or females!
Question:
I'm talking about contraceptive drugs
Answers:
I am no expert on the subject but there are gonadotropin antagonists available already (I know you are suggesting an FSH blocker) See the discussion below:
A gonadotropin-reelasing hormone antagonist (GnRH antagonist) is a synthetic peptide that competes with the neurohormone GnRH for its receptor, thus decreasing or blocking GnRH action. As a result endogenous pituitary output of FSH and LH is shut down.
"GnRH antagonists are also derivatives of the natural GnRH decapeptide with multiple amino acid substitutions. These substitutions modify the agent so that it blocks the receptor and decreases FSH and LH secretions within hours. In contrast to GnRH agonists, antagonists have no flare effect, thus their therapeutic effect is immediately apparent. However, there action is short-lived and daily injections are necessary to maintain their effect. Typically endogenous FSH and LH activity returns about 40 hours after cessation of GnRH antagonist administration, although with a higher dose the return to normal pituitary function will be postponed for longer. Unlike the GnRH agonists, long acting or depot forms of the agent are not available, thus GnRH agonists are not used in the long term therapy of patients with cancer where hormone levels need to be kept low for a long time.
The main application of GnRH agonists is currently short term use in the prevention of endogenous ovulation in patients who undergo exogenous stimulation with FSH in the preparation for IVF. Typically they are administered in the mid- to late follicular phase in stimulated cycles prior to the administration of hCG. Because they decrease luteal competence, patients are usually given some form of luteal support after egg retrieval.
GnRH agonists for long term use are under investigation (i.e. abarelix), their adavantage over GnRH agonist would be that they lack the initial flare stimulation and induce quickly a [hypogonadal situation.
FDA-approved medications are used by as injectables:
Cetrorelix acetate (Cetrotide), by Serono
Ganirelix acetate (Antagon), by Organon.
Abarelix
GnRH antagonists are pregnancy category X agents."
Here is a version of agonist
"A gonadotropin-releasing hormone agonist (GnRH agonist) is a synthetic peptide modeled after the hypothalamic neurohormone GnRH that interacts with its receptor to elicit its biologic response, the release of the pituitary hormones FSH and LH. Agonists do not quickly dissociate from the GnRH receptor. As a result initially there is an increase in FSH and LH secretion (so-called flare effect), however after about ten days a profound hypogonadal effect is achieved through receptor downregulation. Generally this induced and reversible hypogonadism is the therapeutic goal.
GnRH agonists are synthetically modeled after the natural GnRH decapeptide with specific amino acid substitutions typically in position 6 and 10. These substitutions inhibit rapid degradation. Agonists with 2 substitutions include:
leuprolide (Lupron, Eligard),
buserelin (Suprefact, Suprecor),
nafarelin (Synarel),
historelin,
goserelin (Zoladex),
deslorelin."
It is an interesting idea but it would be hard to imagine this has either been tried with negative consequences or there is some barrier to trying like the molecule or receptor have multiple duties.
Other Answers:
Not in males. Yes in females. Side effects are few and far between. (FSH is not present in males!)
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