Potency (pharmacology) in the context of "Antigonadotropin"

In pharmacology, an adjuvant is a drug or other substance, or a combination of substances, that is used to increase the efficacy or potency of certain drugs. Specifically, the term can refer to:

• Adjuvant therapy in cancer management
• Analgesic adjuvant in pain management
• Immunologic adjuvant in vaccines

Muscimol, also known as agarin, pantherine, or pyroibotenic acid, is a GABA_A receptor agonist with sedative and hallucinogenic effects and the principal psychoactive constituent of Amanita mushrooms such as Amanita muscaria (fly agaric) and Amanita pantherina (panther cap). It is a 3-hydroxyisoxazole alkaloid and is closely related structurally to the neurotransmitter γ-aminobutyric acid (GABA). The compound is widely used as a ligand and agonist of the GABA_A receptor in scientific research. Muscimol is typically taken orally, but may also be smoked. Peak effects occur after 1 to 3 hours orally and its duration is 4 to 8 hours but up to 24 hours.

The effects of muscimol in humans include central depression, sedation, sleep, cognitive and motor impairment, hallucinations, perceptual distortion, and muscle twitching, among others. Muscimol acts as a potent GABA_A receptor full agonist. It is also a potent GABA_A-ρ receptor partial agonist and a weak GABA reuptake inhibitor. The drug is inactive at the GABA_B receptor but is a substrate of GABA transaminase (GABA-T). Muscimol mostly exerts its effects via GABA_A receptor activation. It is very different from drugs like benzodiazepines and barbiturates as it is an orthosteric agonist of the GABA_A receptor rather than an allosteric modulator. Unlike GABA, muscimol crosses the blood–brain barrier and hence is centrally active. Muscimol, which is also known chemically as 5-aminomethylisoxazol-3-ol, is a conformationally restrained analogue of GABA. The related compound and Amanita spp. constituent ibotenic acid is a prodrug of muscimol.

Gaboxadol, also known as 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP) and by its former developmental code names Lu-2-030, MK-0928, and OV101, is a GABA_A receptor agonist related to muscimol which was investigated for the treatment of insomnia and other conditions like Angelman syndrome but was never marketed. At lower doses, the drug has sedative and hypnotic effects, and at higher doses, it produces hallucinogenic effects. It is taken orally.

The drug acts as a potent and selective partial agonist of the GABA_A receptor, the major signaling receptor of the inhibitory endogenous neurotransmitter γ-aminobutyric acid (GABA). However, it acts as a preferential supra-maximal agonist at extrasynaptic δ subunit-containing GABA_A receptors. In contrast to GABA_A receptor positive allosteric modulators like benzodiazepines and Z drugs, gaboxadol is an orthosteric agonist of the GABA_A receptor, acting on the same site as GABA rather than at an allosteric regulatory site. As a result, gaboxadol has differing effects from benzodiazepines and related drugs. Gaboxadol is a conformationally constrained synthetic analogue of GABA and of muscimol, an alkaloid and hallucinogen found in Amanita muscaria (fly agaric) mushrooms. It has greatly improved drug-like properties compared to these compounds.

A lead compound (/ˈliːd/, i.e., a "leading" compound; not to be confused with various compounds of the element lead) in drug discovery is a chemical compound that has pharma­co­logical or biological activity likely to be therapeutically useful, but may never­the­less have suboptimal structure that requires modification to fit better to the target; lead drugs offer the prospect of being followed by "back-up" compounds. The chemical structure serves as a starting point for chemical modifications in order to improve potency, selectivity, or pharma­co­kinetic parameters. Furthermore, newly-invented pharma­co­logically active moieties may have poor druglikeness and may require chemical modification to become "drug-like" enough to be tested biologically or clinically.

Lead compounds are sometimes called developmental candidates. This is because the discovery and selection of lead compounds occurs prior to preclinical and clinical development of the candidate.

3-Iodothyronamine (T₁AM) is an endogenous thyronamine. It is a high-affinity ligand of the trace amine-associated receptor 1 (TAAR1). T₁AM is the most potent endogenous TAAR1 agonist yet discovered. It is also an agonist of the TAAR2 and TAAR5 with similar potency as for the TAAR1 (all in the case of the human proteins). T₁AM is not a ligand of the thyroid hormone receptors. However, it is additionally a ligand of various monoamine and other receptors. For instance, it is a muscarinic acetylcholine receptor antagonist.