1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor

TCB2 

Cat. No.: HY-103102
Handling Instructions

TCB2 is an agonist of serotonin 5-HT2A receptor.

For research use only. We do not sell to patients.

TCB2 Chemical Structure

TCB2 Chemical Structure

CAS No. : 912342-28-0

Size Stock
250 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

TCB2 is an agonist of serotonin 5-HT2A receptor.

IC50 & Target

5-HT2A Receptor

 

In Vitro

The selective 5-HT2A agonist TCB2 at 30 nM produces a marked shift to the right in the competition curve obtained with the 5-HT1A receptor agonist ipsapirone from [3H]-8-OHDPAT binding sites in both areas of the brain. A significant increase in the mean Ki value is obtained with TCB2, demonstrating a reduction in the affinity of the high-affinity 5-HT1A agonist binding sites by the 5-HT2A agonist in both regions. In the case of hippocampus, there are also indications for antagonistic effects of ketanserin[2].

In Vivo

In an initial dose-response study, TCB2 (0.5, 1.0, and 2.5 mg/kg) and DOI (0.5, 1.0, 2.5, and 5.0 mg/kg) induce head twitches in C57BL/6J mice in a dose-dependent manner compared to vehicle. Head twitches induced by TCB2 and DOI are similar across the doses, with the exception that at the highest dose (5.0 mg/kg), TCB2 induces half as many head twitches as does DOI (p=0.021). Confirming 5-HT2A mediation of the head twitch response, in two separate studies, pretreatment with the selective 5-HT2A antagonist MDL 11,939 (1.0 mg/kg) block head twitches induced by DOI (2.5 mg/kg) and by TCB2 (2.5 mg/kg; p<0.0001). Compared to vehicle, corticosterone levels are increased following TCB2 (5.0 mg/kg, p=0.01; 10.0, p=0.012; with a trend following 2.5 mg/kg, p=0.079) and DOI (10.0 mg/kg, p=0.035)[1].

Solvent & Solubility
In Vitro: 

10 mM in H2O

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8325 mL 14.1623 mL 28.3246 mL
5 mM 0.5665 mL 2.8325 mL 5.6649 mL
10 mM 0.2832 mL 1.4162 mL 2.8325 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]
Male C57BL/6J mice and SERT+/+ (+/−, −/−) mice (25-30 g) are used. TCB2 is dissolved in distilled water, MDL 11,939 is dissolved in a few drops of acetic acid and prepared in distilled water, and DOI is dissolved in saline. All drugs and their vehicles are administered via intraperitoneal injection at a volume of 10 ml/kg. Following 15 min of habituation in a plexiglass container, mice are administered the test drug. Head twitches were recorded for five 1-min periods over a 30-min period; the scores from the five 1-min periods are summed together. In two separate experiments, mice are pretreated with the selective 5-HT2A antagonist MDL 11,939 (1.0 mg/kg) or its vehicle 30 min prior to administration of DOI or TCB2 (2.5 mg/kg). Finally, head twitches are assessed in SERT+/+ (+/−, −/−) mice administered TCB2. C57BL/6J mice are injected with vehicle, TCB2 (1.0 or 2.5 mg/kg) or DOI (1.0 or 2.5 mg/kg). Following administration of vehicle, TCB2 (1.0, 2.5, or 5.0 mg/kg) or DOI (1.0, 2.5, or 5.0 mg/kg), mice are placed in the test cage. In a final feeding study, mice are pretreated with vehicle or MDL 11,939 (1.0 mg/kg) followed 30 min later by an intermediate dose of TCB2 (3.75 mg/kg)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

353.05

Formula

C₁₁H₁₅Br₂NO₂

CAS No.

912342-28-0

SMILES

NCC1C2=C(OC)C=C(Br)C(OC)=C2C1.[H]Br

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
TCB2
Cat. No.:
HY-103102
Quantity:

TCB2

Cat. No.: HY-103102