Adrenergic Receptors in the Ptotic Human Eyelid: Correlation With Phenylephrine Testing and Surgical Success in Ptosis Repair

Skibell, Bentley C.; Harvey, John H.; Oestreicher, James H.; Howarth, David; Gibbs, Alison L.; Wegrynowski, Trish; Wing, T W; DeAngelis, Dan

doi:10.1097/iop.0b013e3181462a2e

Cited by 46 publications

(24 citation statements)

References 14 publications

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“…These behavioral changes presumably are mediated by the blocking of histamine H 1 receptor or ␣ 1 receptor (Skibell et al, 2007), and these results are in agreement with in vitro receptor binding profiles that lurasidone has relatively low affinity for noradrenergic ␣ 1 receptor or negligible affinity for histamine H 1 receptor. These findings suggested that lurasidone would have fewer risks of cardiovascular side effects, such as orthostatic hypotension, and CNS depressant side effects, such as sedation or somnolence.…”

Section: Discussionsupporting

confidence: 74%

Pharmacological Profile of Lurasidone, a Novel Antipsychotic Agent with Potent 5-Hydroxytryptamine 7 (5-HT₇) and 5-HT_1A Receptor Activity

Ishibashi¹,

Horisawa²,

Tokuda³

et al. 2010

J Pharmacol Exp Ther

385

304

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Lurasidone [(3aR,4S,7R,7aS)-2-{(1R,2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1-ylmethyl]cyclohexylmethyl}hexahydro-4,7-methano-2H-isoindole-1,3-dione hydrochloride; SM-13496] is an azapirone derivative and a novel antipsychotic candidate. The objective of the current studies was to investigate the in vitro and in vivo pharmacological properties of lurasidone. Receptor binding affinities of lurasidone and several antipsychotic drugs were tested under comparable assay conditions using cloned human receptors or membrane fractions prepared from animal tissue. Lurasidone was found to have potent binding affinity for dopamine D 2 , 5-hydroxytryptamine 2A (5-HT 2A ), 5-HT 7 , 5-HT 1A , and noradrenaline ␣ 2C receptors. Affinity for noradrenaline ␣ 1 , ␣ 2A , and 5-HT 2C receptors was weak, whereas affinity for histamine H 1 and muscarinic acetylcholine receptors was negligible. In vitro functional assays demonstrated that lurasidone acts as an antagonist at D 2 and 5-HT 7 receptors and as a partial agonist at the 5-HT 1A receptor subtype. Lurasidone showed potent effects predictive of antipsychotic activity, such as inhibition of methamphetamine-induced hyperactivity and apomorphine-induced stereotyped behavior in rats, similar to other antipsychotics. Furthermore, lurasidone had only weak extrapyramidal effects in rodent models. In animal models of anxiety disorders and depression, treatment with lurasidone was associated with significant improvement. Lurasidone showed a preferential effect on the frontal cortex (versus striatum) in increasing dopamine turnover. Anti-␣ 1 -noradrenergic, anticholinergic, and central nervous system (CNS) depressant actions of lurasidone were also very weak. These results demonstrate that lurasidone possesses antipsychotic activity and antidepressant-or anxiolytic-like effects with potentially reduced liability for extrapyramidal and CNS depressant side effects.

show abstract

Section: Discussionsupporting

confidence: 74%

Pharmacological Profile of Lurasidone, a Novel Antipsychotic Agent with Potent 5-Hydroxytryptamine 7 (5-HT₇) and 5-HT_1A Receptor Activity

Ishibashi¹,

Horisawa²,

Tokuda³

et al. 2010

J Pharmacol Exp Ther

385

304

View full text Add to dashboard Cite

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“…20 However, eyelid elevation response to phenylephrine was not correlated with the amount of the receptors, consistent with this study. The authors found that the effect of phenylephrine was inversely related to the amount of α 2C -adrenoceptor staining.…”

Section: Discussionsupporting

confidence: 82%

Selective α_1A-Adrenoceptor Stimulation Induces Mueller’s Smooth Muscle Contraction in an Isolated Canine Upper Eyelid Preparation

Yano¹,

Hirose²,

Nakada³

et al. 2010

Current Eye Research

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“…Revision of the literature on etiologies responsible for the signs present in the Horner's syndrome revealed a number of diseases specifically associated with Horner's syndrome, such as Pancoast tumor of the lung (Attar et al 1998), Rowlend-Payne syndrome, caused by mediastinal neuroblastoma (Kapoor et al 2005), pseudoaneurysm of the internal carotid artery (Mastan 2005), metastatic breast cancer (Kovacic et al 2007), some congenital lesions (Castillo et al 2005;Gupta et al 2005) and metastatic tumor of the cavernous sinus (Tsuda et al 2005). Sympathetic fibers with adrenergic receptors alpha-1D, alpha-2C and beta-2 receptors have been documented within human STM, and the alpha-2C receptor in particular may play a role in determining the response of the eyelid to phenylephrine (Skibell et al 2007).…”

Section: Discussionmentioning

confidence: 99%

The human superior tarsal muscle (Müller’s muscle): a morphological classification with surgical correlations

et al. 2009

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The superior tarsal muscle (STM) is a smooth muscle that originates from the undersurface of the levator palpebrae superioris muscle (LPSM) and inserts onto the superior tarsal plate (STP) of the upper eyelid. We have performed a morphometrical investigation of the STM in 49 adult human cadavers (34 males, 15 females). Histological analysis has shown a transitional area between the skeletal striated muscle (LPSM) and the adjacent smooth muscle (STM). We propose an original morphological classification based upon the attachment of STM to the upper border of the STP. Accordingly, we describe four patterns of STM. Pattern 1 (P1) consists of STM attachment to the central portion of the STP. Pattern 2 consists of both medial (P2M) STM attachment to both the central and medial regions of the STP and lateral (P2L) STM attachment to both the central and lateral regions of the STP. Pattern 3 (P3) consists of STM attachment along the whole extent of the STP. Pattern 3 was the most frequently observed pattern (63.27%) followed by patterns P2M (24.49%), P2L (8.16%) and P1 (4.08%). P3 was the predominant pattern in males (73.52%), while in females, both patterns P2M (46.66%) and P3 (40.00%) were equally prevalent. The analysis of paired specimens revealed a symmetrical arrangement in 72.20% of all cases, with the remaining cases (27.80%) displaying left-right STM asymmetries. To the best of our knowledge, this is the first description of the STM asymmetries in the medical literature. This innovative classification provides anatomical parameters for interpreting morphological variations of the STM with relevant applications in both plastic surgery and ophthalmology.

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Adrenergic Receptors in the Ptotic Human Eyelid: Correlation With Phenylephrine Testing and Surgical Success in Ptosis Repair

Cited by 46 publications

References 14 publications

Pharmacological Profile of Lurasidone, a Novel Antipsychotic Agent with Potent 5-Hydroxytryptamine 7 (5-HT₇) and 5-HT_1A Receptor Activity

Pharmacological Profile of Lurasidone, a Novel Antipsychotic Agent with Potent 5-Hydroxytryptamine 7 (5-HT₇) and 5-HT_1A Receptor Activity

Selective α_1A-Adrenoceptor Stimulation Induces Mueller’s Smooth Muscle Contraction in an Isolated Canine Upper Eyelid Preparation

The human superior tarsal muscle (Müller’s muscle): a morphological classification with surgical correlations

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Adrenergic Receptors in the Ptotic Human Eyelid: Correlation With Phenylephrine Testing and Surgical Success in Ptosis Repair

Cited by 46 publications

References 14 publications

Pharmacological Profile of Lurasidone, a Novel Antipsychotic Agent with Potent 5-Hydroxytryptamine 7 (5-HT7) and 5-HT1A Receptor Activity

Pharmacological Profile of Lurasidone, a Novel Antipsychotic Agent with Potent 5-Hydroxytryptamine 7 (5-HT7) and 5-HT1A Receptor Activity

Selective α1A-Adrenoceptor Stimulation Induces Mueller’s Smooth Muscle Contraction in an Isolated Canine Upper Eyelid Preparation

The human superior tarsal muscle (Müller’s muscle): a morphological classification with surgical correlations

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Product

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Pharmacological Profile of Lurasidone, a Novel Antipsychotic Agent with Potent 5-Hydroxytryptamine 7 (5-HT₇) and 5-HT_1A Receptor Activity

Pharmacological Profile of Lurasidone, a Novel Antipsychotic Agent with Potent 5-Hydroxytryptamine 7 (5-HT₇) and 5-HT_1A Receptor Activity

Selective α_1A-Adrenoceptor Stimulation Induces Mueller’s Smooth Muscle Contraction in an Isolated Canine Upper Eyelid Preparation