Pharmacology of N-, L-, and B-subtypes of nematode nAChR resolved at the single-channel level in Ascaris suum.

Pharmacology of N-, L-, and B-subtypes of nematode nAChR resolved at the single-channel level in Ascaris suum. Research Abstract Details 

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Pharmacology of N-, L-, and B-subtypes of nematode nAChR resolved at the single-channel level in Ascaris suum. Abstract Text:

Hai Qian,Richard J Martin,Alan P Robertson,

Pharmacological experiments on Ascaris suum have demonstrated the presence of three (N-, L-, and B-) subtypes of cholinergic receptor mediating contraction of body wall muscle in parasitic nematodes. In the present study, these ionotropic acetylcholine (ACh) receptors (nAChRs) were activated by levamisole and bephenium under patch-clamp conditions and competitively antagonized by paraherquamide and 2-desoxoparaherquamide. A number of recordings exhibited three separate current amplitude levels, indicating the presence of small, intermediate, and large conductance subtypes of receptor. The mean conductance of the small conductance subtype, G25, was 22 +/- 1 pS; the intermediate conductance channel, G35, was 33 +/- 1 pS; and the large conductance channel, G45, was 45 +/- 1 pS. The small channel was not antagonized significantly by paraherquamide and was identified as the N-subtype. The intermediate channel was preferentially activated by levamisole rather than bephenium and antagonized by paraherquamide: the intermediate channel was identified as the L-subtype. The large conductance channel was preferentially activated by bephenium, antagonized more by 2-desoxoparaherquamde than by paraherquamide and was identified as the B-subtype. These observations reveal that the three channel subtypes have different selectivity for cholinergic anthelmintics. The different selectivity of these compounds should be considered when dealing with drug resistant infections.

Pharmacology of N-, L-, and B-subtypes of nematode nAChR resolved at the single-channel level in Ascaris suum. Publishing Authors By Initials

H Qian,RJ Martin,AP Robertson,

For similar organic chemicals: hydrocarbons: hydrocarbons, cyclic: hydrocarbons, aromatic: polycyclic hydrocarbons, aromatic: spiro compounds research abstracts see: organic chemicals: hydrocarbons: hydrocarbons, cyclic: hydrocarbons, aromatic: polycyclic hydrocarbons, aromatic: spiro compounds research

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Pharmacology of N-, L-, and B-subtypes of nematode nAChR resolved at the single-channel level in Ascaris suum. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: The FASEB journal : official publication of the Fe

VOLUME: 20

Page Numbers: 2606-8

Journal Abbreviation: FASEB J.

ISSN: 1530-6860

DAY: 20

MONTH: 10

YEAR: 2006

Pharmacology of N-, L-, and B-subtypes of nematode nAChR resolved at the single-channel level in Ascaris suum. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 8804484

Pharmacology of N-, L-, and B-subtypes of nematode nAChR resolved at the single-channel level in Ascaris suum. Keywords Mesh Terms:

KEYWORDS: Spiro Compounds

MESH TERMS: pharmacology

Chemical & Substance for Abstract: Pharmacology of N-, L-, and B-subtypes of nematode nAChR resolved at the single-channel level in Ascaris suum. Information

Substance Name: paraherquamide

Registry Number: 77392-58-6

Grant and Affiliation Information for Pharmacology of N-, L-, and B-subtypes of nematode nAChR resolved at the single-channel level in Ascaris suum.

AFFILIATION: Department of Biomedical Sciences, College of Veterinary Medicine, Iowa State University, Ames, Iowa 50011-1250, USA.

Country: United States

AGENCY: United States NIAID

GRANT: R01 AI47194

ACRONYM: AI

MEDLINETA: FASEB J

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