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goitrin

compound / compound-goitrin

ゴイトリン

Goitrin is a cyclic hydrolysis product of the glucosinolate progoitrin; an agonist of the human TAS2R38 bitter taste receptor.

On this page (7 sections)
  1. Overview
  2. Sources for this overview (3)
  3. Topic hubs
  4. Follow the connections
  5. Related entries (10)
  6. Sensory (1)
  7. Mechanism and receptors (2)
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Reading the bitterness

Goitrin is a substance produced by hydrolysis of progoitrin from the Brassica family and is being tested as an agonist of the human TAS2R38 bitter taste receptor. In allele-specific in vitro assays performed with 56 subjects after confirming genetic diversity, phenylthiocarbamide (PTC), propylthiouracil (PROP), and methimazole, together with goitrin and sinigrin, were also tested as TAS2R38 agonists, and the response showed a continuous range across alleles. The relationship between threshold and genotype was strongly significant (P<0.005) for all three single nucleotide polymorphisms in the thiourea compounds PTC, PROP, goitrin, and methimazole, and was also significant (P<0.001) for the PAV/AVI haplotype. However, only sinigrin was measured in 25 subjects in a subgroup, and although significant, the P value was higher (0.03–0.04), and the authors themselves noted the limitations of power from the small sample. The rank order of efficacy for each compound cannot be discerned from this material.

The axis of allele-dependent function of TAS2R38 is supported by separate independent research. In functional expression and calcium imaging of 8 constructed TAS2R38 receptors (of which 5 natural haplotypes), the PAV-type receptor responded to PTC with half-maximal effective concentration of 1.1 micromolar, to PROP with 2.1 micromolar, while the AVI-type did not respond to either PTC or PROP even at the high concentration of 1 millimolar, as reported. However, in this research, goitrin and sinigrin themselves were not tested; what can be confirmed here only independently supports the axis of allele-dependent function of TAS2R38 as demonstrated by PTC and PROP.

Within the scope of the abstract, goitrin's response to the PAV-type (responsive-type) allele of TAS2R38 was EC50 65.0 micromolar, weaker than PROP (EC50 2.1 micromolar) or PTC (EC50 1.1 micromolar) in the same assay. No response was obtained from the AVI-type (non-responsive-type) allele.

In psychophysical threshold measurement in 50 subjects, threshold response to goitrin showed a significant correlation with both response to PROP (P=8.9×10⁻⁴, rs=0.46) and response to PTC (P=7.5×10⁻⁴, rs=0.46) (within the scope of the abstract). The proportion of variance in goitrin response explained by TAS2R38 genetic variation was r²=0.16, smaller than for PROP (r²=0.50) or PTC (r²=0.57).

Sources for this overview

  1. Genetic, functional, and phenotypic diversity in TAS2R38-mediated bitter taste perception

    Behrens M; Gunn HC; Ramos PC; Meyerhof W; Wooding SP / 2013 / journal article / full text checked

    Checked for this overview: Used as evidence for goitrin agonist assay results in 56 subjects.

  2. The molecular basis of individual differences in phenylthiocarbamide and propylthiouracil bitterness perception

    Bufe B; Breslin PA; Kuhn C; Reed DR; Tharp CD; Slack JP; Kim UK; Drayna D; Meyerhof W / 2005 / journal article / full text checked

    Checked for this overview: Used as evidence for allele-specific receptor function as shown by EC50 difference between PAV-type and AVI-type.

  3. Genetics and bitter taste responses to goitrin, a plant toxin found in vegetables

    Wooding S; Gunn H; Ramos P; Thalmann S; Xing C; Meyerhof W / 2010 / journal article / abstract checked

    Checked for this overview: Comparison of goitrin EC50 values for PAV-type and AVI-type alleles with those of PROP and PTC. / Numerical values for threshold response in 50 subjects and variance explained by TAS2R38 genetic variation.

Follow the connections

TAS2R38 →is activated in vitro by→ goitrin

goitrin →activates→ TAS2R38 →modulates the perceived int…→ bitterness

Structured claims — open a section to read each claim's confidence, evidence and limits

Sensory (1)

goitrin — perceived bitterness is associated with: TAS2R38preliminary

Scope: Layer: solution (psychophysical threshold measurement). A study of 50 subjects examining the association between threshold taste responses to goitrin, PROP, and PTC, and TAS2R38 genotype/functional variants.

Note: Confirmed at abstract level only. A quantitative finding showing that TAS2R38 genetic variation alone cannot explain most of the variance in goitrin response (the authors suggest the involvement of other factors).

"threshold responses to goitrin were associated with responses to both PROP (P = 8.9 x 10(-4); r(s) = 0.46) and PTC (P = 7.5 x 10(-4); r(s) = 0.46)... goitrin responses were significantly associated with mutations in TAS2R38 (P = 9.3 x 10(-3)), but the same mutations accounted for a smaller proportion of variance in goitrin response (r(2) = 0.16) than for PROP (r(2) = 0.50) and PTC (r(2) = 0.57)."
Limitations: Confirmed at abstract level. Both the correlation coefficient (rs) and the variance-explained figure (r2) are given together; the threshold's own absolute value (concentration) is not stated in the abstract.
Source: Genetics and bitter taste responses to goitrin, a plant toxin found in vegetables (Wooding S; Gunn H; Ramos P; Thalmann S; Xing C; Meyerhof W, 2010) · abstract checked
Show datacompound-goitrin —has_perceived_bitterness_associated_with→ receptor-tas2r38
claim: clm-w71a1-goitrin-threshold-correlates-prop-ptc / type: sensory / updated: 2026-09-07

Mechanism and receptors (2)

TAS2R38goitrin is activated in vitro by: supported

Scope: Allele-specific in vitro functional assay of the 6 TAS2R38 haplotypes, confirmed by full-gene sequencing in 56 white subjects

Note: Gives a receptor-level link connecting Brassica glucosinolate chemistry to the PROP/PTC sensitivity axis. The abstract has no per-compound EC50 or threshold values, so a potency ranking is not recorded.

Genetic diversity was confirmed by full-gene sequencing in 56 white subjects, and allele-specific responses to 5 TAS2R38 agonists (PTC, PROP, goitrin, methimazole, and sinigrin) were analyzed by in vitro assay. However, the number of subjects for detection-threshold measurement differed by compound: all 56 subjects for salicin, PTC, PROP, goitrin, and methimazole, but only 25 (a subpopulation) for sinigrin. The genotype association with threshold was strongly significant for PTC/PROP/goitrin/methimazole (the thioamide compounds), at P<0.005 and β>1.85 for all 3 SNPs, whereas for sinigrin all 3 SNPs were significant but with higher P-values (0.04, 0.03, 0.03), and the authors themselves state that power is limited by the small sample of N=25. The P<0.001 for the PAV/AVI haplotype is mainly the value for the thioamide compounds.
Limitations: It should be noted explicitly that the genotype–threshold association for sinigrin is statistically weaker than for the thioamide compounds and comes from a small sample (N=25).
Source: Genetic, functional, and phenotypic diversity in TAS2R38-mediated bitter taste perception (Behrens M; Gunn HC; Ramos PC; Meyerhof W; Wooding SP, 2013) · full text checked
Verbatim: 'Functional expression studies demonstrate that five different haplotypes from the hTAS2R38 gene code for operatively distinct receptors.' The PAV receptor responded with an EC50 of 1.1 uM (PTC) and 2.1 uM (PROP), while 'hTAS2R38-AVI did not respond to PTC or PROP concentrations as high as 1 mM.' PVI, AAI, and AAV responded with EC50 values close to PAV. Concentration–intensity functions and recognition thresholds were measured in 32 subjects of known TAS2R38 diplotype, and one PAV subject's lowest discriminable concentration corresponded to the PAV receptor's in vitro EC50.
Limitations: This study did not test goitrin or sinigrin, so it independently supports the allele-dependent TAS2R38 function axis of this claim (via PTC/PROP), but does not itself support goitrin/sinigrin agonism.
Source: The molecular basis of individual differences in phenylthiocarbamide and propylthiouracil bitterness perception (Bufe B; Breslin PA; Kuhn C; Reed DR; Tharp CD; Slack JP; Kim UK; Drayna D; Meyerhof W, 2005) · full text checked
Context: The full-text Discussion of Eib et al. (2020) mentions the relationship between sinigrin's bitterness and TAS2R38. Verbatim: "Sinigrin is associated with bitterness; this is a basic taste, which is predominantly perceived via the TASTE 2 receptor (TAS2R) family on the tongue (Bell et al., 2018). In particular, sinigrin binds preferably to TAS2R38 (Meyerhof, Kuhn, Chudoba, et al., 2010)." This is not Eib's own measurement but a secondary mention citing the receptor-preference finding of Meyerhof et al. 2010.
Limitations: The primary data are in the Meyerhof 2010 TAS2R source. That source currently has access_status=restricted and review_status=abstract_checked, and the sources.csv notes do not yet mention sinigrin. This line follows the pattern of 『別ソース全文で見つかった一次文献への二次引用』 (in translation: "a secondary citation, within the full text of a different source, to primary literature found there"); once the full text of Meyerhof 2010 itself becomes readable, this line should be replaced with a primary evidence line, or treated, for now, as a provisional secondary citation that needs to be supplemented.
Source: Determination of detection thresholds of sinigrin in water-based matrix and allyl isothiocyanate in water- and oil-based matrices (Eib Sabrina; Ramos Gajek Sarah; Schneider Desiree Janet; Hensel Oliver; Seuss-Baum Ingrid, 2020) · full text checked
Context: In vitro, allelic differences in EC50 for each agonist were not statistically significant, whereas the magnitude of the response (ΔF/F) within the same agonist differed greatly between alleles. PAV responded strongly to all agonists, and AVI did not respond above baseline to any of them. Verbatim: "allelic differences in EC50 within agonists were not statistically significant. In contrast, within-agonist comparisons revealed highly divergent functionality among alleles as measured by ΔF/F."
Limitations: The lack of a significant difference in EC50 may partly reflect a power issue. The correspondence with human thresholds is covered in a separate section of the main text.
Source: Genetic, functional, and phenotypic diversity in TAS2R38-mediated bitter taste perception (Behrens M; Gunn HC; Ramos PC; Meyerhof W; Wooding SP, 2013) · full text checked
Show datareceptor-tas2r38 —is_activated_in_vitro_by→ compound-goitrin
claim: clm-goitrin-sinigrin-tas2r38-agonists / type: mechanism / updated: 2026-08-30
goitrin activates TAS2R38preliminary

Scope: Layer: cell. Comparison of EC50 values for goitrin, PROP, and PTC by TAS2R38 functional expression assay. Part of a study examining the relationship to taste-threshold responses in 50 subjects.

"goitrin elicits a weaker response from the sensitive (PAV) allele of TAS2R38 (EC(50) = 65.0 microM) than do either PROP (EC(50) = 2.1 microM) or PTC (EC(50) = 1.1 microM) and no response at all from the insensitive (AVI) allele."
Limitations: Confirmed at abstract level. Details of assay methodology (detection method, etc.) are not described in the abstract.
Source: Genetics and bitter taste responses to goitrin, a plant toxin found in vegetables (Wooding S; Gunn H; Ramos P; Thalmann S; Xing C; Meyerhof W, 2010) · abstract checked
Show datacompound-goitrin —activates→ receptor-tas2r38
claim: clm-w71a1-goitrin-tas2r38-pav-ec50 / type: mechanism / updated: 2026-09-07

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