SB 216641 hydrochloride - CAS 193611-67-5
Category: Inhibitor
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Molecular Formula:
C28H30N4O4.HCl
Molecular Weight:
523.03
COA:
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Targets:
5-HT Receptor
Description:
SB 216641 hydrochloride is a selective h5-HT1B antagonist with ~ 25-fold selectivity over h5-HT1D and little or no affinity for a range of other receptor types.
Brife Description:
h5-HT1B antagonist
Purity:
≥98% by HPLC
Related CAS:
170230-39-4 (free base)
Synonyms:
SB 216641 hydrochloride; SB216641 hydrochloride; SB-216641 hydrochloride; N-[3-[3-(Dimethylamino)ethoxy]-4-methoxyphenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-carboxamide hydrochloride
MSDS:
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InChIKey:
JPBMDMNORXKGHZ-UHFFFAOYSA-N
InChI:
InChI=1S/C28H30N4O4.ClH/c1-18-16-22(27-29-19(2)36-31-27)10-12-24(18)20-6-8-21(9-7-20)28(33)30-23-11-13-25(34-5)26(17-23)35-15-14-32(3)4;/h6-13,16-17H,14-15H2,1-5H3,(H,30,33);1H
Canonical SMILES:
CC1=C(C=CC(=C1)C2=NOC(=N2)C)C3=CC=C(C=C3)C(=O)NC4=CC(=C(C=C4)OC)OCCN(C)C.Cl
1.Neonatal DSP-4 treatment impairs 5-HT(1B) receptor reactivity in adult rats. Behavioral and biochemical studies.
Ferdyn-Drosik M;Nowak P;Bojanek K;Bałasz M;Kasperski J;Skaba D;Muchacki R;Kostrzewa RM Pharmacol Rep. 2010 Jul-Aug;62(4):608-20.
To examine the effect of a central noradrenergic lesion on the reactivity of the 5-HT(1B) receptor we compared intact male rats with rats in which noradrenergic nerve terminals were largely destroyed with the neurotoxin DSP-4 (50 mg/kg x 2, on the 1st and 3rd days of postnatal life). When rats attained 10 weeks of age, control and DSP-4 rats were divided into two subgroups receiving either saline or the serotonin (5-HT) synthesis inhibitor (p-chlorophenylalanine; p-CPA; 100 mg/kg). Employing an elevated plus maze test, we demonstrated that CP 94,253 (5-propoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-pyrrolo[3,2-b]pyridine hydrochloride) (4.0 mg/kg; 5-HT(1B) agonist) induced an anxiogenic-like action in control rats; however, it failed to elicit this effect in the DSP-4 group. Surprisingly, in p-CPA pretreated rats anxiogenic-like activity was observed both in control and DSP-4 treated rats. CP 94,253 significantly attenuated 5-HT synthesis in the medial prefrontal cortex (mPFC) of control rats, and SB 216641 (N-{3-[3-(dimethylamino)ethoxy]-4-methoxyphenyl}-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-carboxamide hydrochloride) (4.0 mg/kg; 5-HT(1B) antagonist) was able to antagonize this effect.
2.Role of 5-HT(1B) receptors in the sensitization to amphetamine in mice.
Przegalinski E;Siwanowicz J;Nowak E;Papla I;Filip M Eur J Pharmacol. 2001 Jun 22;422(1-3):91-9.
The present study was designed to determine how 5-HT(1B) receptor ligands affected the development or the expression phase of sensitization to the amphetamine-induced locomotor response in mice. Mice were treated repeatedly (for 5 days) with amphetamine (2.5 mg/kg) in combination with either vehicle, N-[3-[3-(dimethylamino)ethoxy]-4-methoxyphenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-carboxamide hydrochloride (SB 216641; an antagonist of 5-HT(1B) receptors), 3-(1,2,5,6-tetrahydro-4-pyridyl)-5-propoxypyrrolo[3,2-b]pyridine (CP 94,253; an agonist of 5-HT(1B) receptors), or SB 216641+CP 94,253; afterwards, on day 10, they received a challenge dose of amphetamine (2.5 mg/kg). In another experiment, mice were given either vehicle or amphetamine (2.5 mg/kg) for 5 days, and were then challenged with amphetamine (2.5 mg/kg) in combination with vehicle, SB 216641, or CP 94,253 on day 10. Locomotor hyperactivity induced by acute administration of amphetamine (day 1) was dose-dependently inhibited by SB 216641 and enhanced by CP 94,253, but not affected by a combination of SB 216641+CP 94,253. The 5-HT(1B) receptor ligands affected similarly the behavioral response to the challenge dose of amphetamine on day 10 (ca.
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CAS 193611-67-5 SB 216641 hydrochloride

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