Differential effects of β-methylphenylethylamine and octopamine on contractile parameters of the rat gastrointestinal tract

Oliveira, Daniel Pereira de; Oliveira-Silva, Carlos Alberto; Pinheiro, Camila Gadelha; Carvalho, Emanuella Feitosa de; Gadelha, Kalinne Kelly Lima; Lima-Silva, Karine; Cavalcante, Ana Karolina Martins; Belém, Mônica de Oliveira; Paula, Suliana Mesquita; Santos, Armênio Aguiar dos; Magalhães, Pedro Jorge Caldas

doi:10.1016/j.ejphar.2021.174339

Cited by 2 publications

(4 citation statements)

References 34 publications

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“…This was done by examining the effect of EPPTB, a selective TAAR1 antagonist [29] that is structurally related to RO5263397 on TAAR1 agonist-mediated vasodilation in this preparation. EPPTB has been used in several investigations to determine the involvement or otherwise of TAAR1 in a variety of biological actions of trace amines centrally and peripherally [11,23,[30][31][32]. It has been reported that the affinity of EPPTB for TAAR1 exhibits species variation ranging from 0.9 nM in mice through 942 nM in rats and ≥5,000 nM in humans [20].…”

Section: Discussionmentioning

confidence: 99%

“…This is because in a parallel study (to be published), we observed that the increase in perfusion pressure induced by these agonists in kidney preparations not perfused with methoxamine was significantly reduced by EPPTB indicating mediation via TAAR1. Oliveira et al [11] have recently reported that concentration-dependent relaxation of the fundic strip evoked by RO5263397 was not antagonized by EPPTB even at a concentration of 50 μ m , suggesting that TAAR1 activation was not involved in RO5263397-induced relaxation of the fundic strip. The increase in perfusion pressure induced by EPPTB would probably suggest that TAAR1 is constitutively active in the perfused rat kidney preparation, probably playing a significant role in maintaining renal vascular resistance at a low level.…”

Section: Discussionmentioning

confidence: 99%

“…There has been only one study of the pharmacological action of RO5263397 in the periphery. In that study, de Oliveira et al [11] reported that RO5263397 evoked a concentration-dependent relaxation of the rat fundic strip. TAAR1 is also activated by another group of endogenous compounds known as thyronamines.…”

Section: Introductionmentioning

confidence: 98%

“…Batista-Lima et al [24] have reported that β-phenylethylamine, also a TAAR1 agonist, induced relaxation of the rat-isolated gastric fundus strip and that this relaxation was inhibited by the selective TAAR1 antagonist EPPTB (50 µ m ), possibly suggesting mediation of the relaxation response via TAAR1 [25]. However, in the same preparation, relaxation induced by RO5263397, a synthetic selective TAAR1 agonist [5, 8, 9], was not inhibited by EPPTB at the same concentration (50 µ m ) that significantly reduced octopamine- and phenylethylamine-induced relaxation, possibly indicating subtypes of TAAR1 [11, 24]. The main objective of this study was to investigate a possible vasodilator effect of TAAR1 agonists, RO5263397 (synthetic) and T1AM (endogenous), in the isolated perfused rat kidney.…”

Section: Introductionmentioning

confidence: 99%

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Vasodilator Effect of Trace Amines, 3-Iodothyronamine, and RO5263397 in the Rat Perfused Kidney: Comparison with Tryptamine

Jragh¹,

Chandrasekhar²,

Yousif³

et al. 2023

Pharmacology

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Introduction: Trace amine-associated receptors (TAARs) are a family of G protein-coupled receptors and are widely distributed in the body. Activation of TAAR1 by specific agonists can produce a variety of physiological effects centrally and peripherally. The objective of this study was to investigate the vasodilator effect of two selective TAAR1 agonists 3-iodothyronamine (T1AM) and RO5263397 in the isolated perfused rat kidney preparation. Methods: Kidneys were isolated and perfused with Krebs’ solution, gassed with 95% oxygen and 5% carbon dioxide, through the renal artery. Results: In preparations pre-constricted with methoxamine (5 × 10−6<sc>m</sc>), T1AM (10−10 – 10−6 mol), RO5263397 (10−10 – 10−6 mol), and tryptamine (10−10 – 10−6 mol) produced dose-dependent vasodilator responses. EPPTB (1 × 10−6<sc>m</sc>), a selective TAAR1 antagonist, had no effect on vasodilator responses induced by these agonists. A higher concentration of EPPTB (3 × 10−5<sc>m</sc>) produced a sustained increase in perfusion pressure but did not affect vasodilator responses to tryptamine, T1AM, and RO5263397. Agonist-induced vasodilator responses were slightly reduced by the removal of the endothelium but were not affected by L-NAME (1 × 10−4<sc>m</sc>), an inhibitor of nitric oxide synthesis. The vasodilator responses were significantly reduced by inhibiting calcium-activated (tetraethylammonium, 1 × 10−3<sc>m</sc>) and voltage-activated (4-AP, 1 × 10−3<sc>m</sc>) potassium channels. Tryptamine-, T1AM-, and RO5263397-induced vasodilator responses were significantly reduced by BMY7378, a 5-HT1A receptor antagonist. Conclusion: It was concluded that vasodilator responses produced by the TAAR1 agonists, T1AM, RO5263397, and tryptamine, were not mediated via TAAR1 but were probably via activation of 5-HT1A receptors.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 98%

Section: Introductionmentioning

confidence: 99%

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Vasodilator Effect of Trace Amines, 3-Iodothyronamine, and RO5263397 in the Rat Perfused Kidney: Comparison with Tryptamine

Jragh¹,

Chandrasekhar²,

Yousif³

et al. 2023

Pharmacology

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Dopamine Receptors and TAAR1 Functional Interaction Patterns in the Duodenum Are Impaired in Gastrointestinal Disorders

Vaganova,

Markina,

Belousov

et al. 2024

Biomedicines

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Currently, there is a growing amount of evidence for the involvement of dopamine receptors and the functionally related trace amine-associated receptor, TAAR1, in upper intestinal function. In the present study, we analyzed their expression in the duodenum using publicly accessible transcriptomic data. We revealed the expression of DRD1, DRD2, DRD4, DRD5, and TAAR1 genes in different available datasets. The results of the gene ontology (GO) enrichment analysis for DRD2 and especially TAAR1 co-expressed genes were consistent with the previously described localization of D2 and TAAR1 in enteric neurons and secretory cells, respectively. Considering that co-expressed genes are more likely to be involved in the same biological processes, we analyzed genes that are co-expressed with TAAR1, DRD2, DRD4, and DRD5 genes in healthy mucosa and duodenal samples from patients with functional dyspepsia (FD) or diabetes-associated gastrointestinal symptoms. Both pathological conditions showed a deregulation of co-expression patterns, with a high discrepancy between DRDs and TAAR1 co-expressed gene sets in normal tissues and patients’ samples and a loss of these genes’ functional similarity. Meanwhile, we discovered specific changes in co-expression patterns that may suggest the involvement of TAAR1 and D5 receptors in pathologic or compensatory processes in FD or diabetes accordingly. Despite our findings suggesting the possible role of TAAR1 and dopamine receptors in functional diseases of the upper intestine, underlying mechanisms need experimental exploration and validation.

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Differential effects of β-methylphenylethylamine and octopamine on contractile parameters of the rat gastrointestinal tract

Cited by 2 publications

References 34 publications

Vasodilator Effect of Trace Amines, 3-Iodothyronamine, and RO5263397 in the Rat Perfused Kidney: Comparison with Tryptamine

Vasodilator Effect of Trace Amines, 3-Iodothyronamine, and RO5263397 in the Rat Perfused Kidney: Comparison with Tryptamine

Dopamine Receptors and TAAR1 Functional Interaction Patterns in the Duodenum Are Impaired in Gastrointestinal Disorders

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